Search results for: property derivatives

Authors: Kevin A. Droguett, Edwin G. Pérez, Denis Fuentealba, Margarita E. Aliaga, Angélica M. Fierro

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Supramolecular chemistry is a field of growing interest. Moreover, studying the formation of host-guest complexes between macrocycles and dyes is highly attractive due to their potential applications. Examples of the above are drug delivery, catalytic process, and sensing, among others. There are different dyes of interest in the literature; one example is the quinolinone derivatives. Those molecules have good optical properties and chemical and thermal stability, making them suitable for developing fluorescent probes. Secondly, several macrocycles can be seen in the literature. One example is the cucurbiturils. This water-soluble macromolecule family has a hydrophobic cavity and two identical carbonyl portals. Additionally, the thermodynamic analysis of those supramolecular systems could help understand the affinity between the host and guest, their interaction, and the main stabilization energy of the complex. In this work, two 7-(diethylamino) quinoline-2 (1H)-one derivative (QD1-2) and their interaction with cucurbit[7]uril (CB[7]) were studied from an experimental and in-silico point of view. For the experimental section, the complexes showed a 1:1 stoichiometry by HRMS-ESI and isothermal titration calorimetry (ITC). The inclusion of the derivatives on the macrocycle lends to an upward shift in the fluorescence intensity, and the pKa value of QD1-2 exhibits almost no variation after the formation of the complex. The thermodynamics of the inclusion complexes was investigated using ITC; the results demonstrate a non-classical hydrophobic effect with a minimum contribution from the entropy term and a constant binding on the order of 106 for both ligands. Additionally, dynamic molecular studies were carried out during 300 ns in an explicit solvent at NTP conditions. Our finding shows that the complex remains stable during the simulation (RMSD ~1 Å), and hydrogen bonds contribute to the stabilization of the systems. Finally, thermodynamic parameters from MMPBSA calculations were obtained to generate new computational insights to compare with experimental results.

Keywords: host-guest complexes, molecular dynamics, quinolin-2(1H)-one derivatives dyes, thermodynamics

Procedia PDF Downloads 59

Authors: Hubert Pun

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When a manufacturer outsources the production of a product, it distributes its intellectual property (IP) into a supply chain that it may not be able to fully control. An IP agreement between a manufacturer and its suppliers is a popular solution to address the challenge of supplier-copycatting. The goal of this paper is to examine the impact of copycatting, from both the supplier and third-party firms, and the effectiveness of an IP agreement. Specifically, we use a game-theoretic approach to examine a system where a manufacturer outsources to a supplier. The supplier and a third-party firm decide whether or not to enter the market with copycat products while the manufacturer selects the level of marketing investment. The manufacturer can reduce the threat of supplier-copycatting by signing an IP agreement. We find that the manufacturer can be worse off from signing an IP agreement with its supplier, even if the IP agreement is costless and perfectly enforceable. We show that a manufacturer can deter copycat products through vertical integration and IP agreements and we outline the instances where each method is preferred. Furthermore, we find that the manufacturer may choose not to invest in quality improvements as a copycat deterrence strategy. We show that the supplier can benefit from the manufacturer’s decision to sign an IP agreement and that the supplier and the consumers can benefit from government regulations against copycat products. Our paper demonstrates the strengths and limitations of various copycat deterrence strategies when a supplier and third-party may produce copycat products.

Keywords: coopetitive supply chain, copycat, government regulation, intellectual property

Procedia PDF Downloads 153

Authors: Amir Amiri, Naghmeh Morakabati

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During the recent years the six-fold growth of cancer in Iran has led the production of healthy products to become a challenge in the food industry. Due to the young population in the country, the consumption of fast foods is growing. The chemical cancer-causing preservatives are used to produce these products more than the standard; so using an appropriate alternative seems to be important. On the one hand, the plant essential oils show the high antimicrobial potential against pathogenic and spoilage microorganisms and on the other hand they are highly volatile and decomposed under the processing conditions. The study aims to produce the loaded chitosan nanoparticles with different concentrations of savory essential oil to improve the anti-microbial property and increase the resistance of essential oil to oxygen and heat. The encapsulation efficiency was obtained in the range of 32.07% to 39.93% and the particle size distribution of the samples was observed in the range of 159 to 210 nm. The range of Zeta potential was obtained between -11.9 to -23.1 mV. The essential oil loaded in chitosan showed stronger antifungal activity against Rhizopus stolonifer. The results showed that the antioxidant property is directly related to the concentration of loaded essential oil so that the antioxidant property increases by increasing the concentration of essential oil. In general, it seems that the savory essential oil loaded in chitosan particles can be used as a food processor.

Keywords: chitosan, encapsulation, essential oil, nanogel

Procedia PDF Downloads 242

Authors: Jana Tchekalarova, Stela Georgieva, Petia Peneva, Petar Todorov

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In the present study, a series of bioconjugates of N-modified hemorphine analogs containing second pharmacophore cinnamic acids (CA) or caffeic acid (KA) were synthesized by a traditional solid-phase Fmoc chemistry method for peptide synthesis. Electrochemical and fluorometric analysis and in vivo anticonvulsant activity in mice were conducted on the compounds. The three CA (H4-CA, H5-CA, and H7-CA) and three KA (H4-KA, H5-KA, and H7-KA)-conjugated hemorphine derivatives showed dose-dependent anticonvulsant activity in the maximal electroshock test (MES) in mice. The KA-conjugated H5-KA derivate was the only compound that suppressed clonic seizures at the lowest dose of 0.5 µg/mouse in the scPTZ test. The activity against the psychomotor seizures in the 6-Hz test was detected only for the H4-CA (0.5 µg) and H4-KA (0.5 µg and 1 µg), respectively. The peptide derivates did not exhibit neurotoxicity in the rotarod test. Our findings suggest that conjugated CA and KA hemorphine peptides can be used as a background for developing hemorphin-related analogs with anticonvulsant activity. Acknowledgments: This study is funded by the European Union-NextGenerationEU, through the National Recovery and Resilience Plan of the Republic of Bulgaria, project № BG-RRP-2.004-0002, "BiOrgaMCT".

Keywords: hemorphins, SPSS, caffeic/cinnamic acid, anticonvulsant activity, electrochemistry, fluorimetry

Procedia PDF Downloads 126

Authors: Nadine Wills

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The whole life thinking of buildings (independent if these are commercial properties or residential properties) will raise if incentive systems are provided to investors, planners and users. The Use of Building Information Modelling (BIM)-Systems offers planners the possibility to plan and re-plan buildings for decades after a period of utilization without spending many capacities. The strategy-incentive should be to plan the building in a way that makes rescheduling possible by changing just parameters in the system and not re-planning the whole building. If users receive the chance to patient incentive systems, the building stock will have a long life period. Business models of tenant electricity or self-controlled operating costs are incentive systems for building –users to let fixed running costs decline without producing damages due to wrong purposes. BIM is the controlling body to ensure that users do not abuse the incentive solution and take negative influence on the building stock. The investor benefits from the planner’s and user’s incentives: the fact that the building becomes useful for the whole life without making unnecessary investments provides possibilities to make investments in different assets. Moreover, the investor gains the facility to achieve higher rents by merchandise the property with low operating costs. To execute BIM offers whole property life cycles.

Keywords: BIM, incentives, life cycle, sustainability

Procedia PDF Downloads 271

Authors: Barna Arnold Keserű

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In the last few years (what is called by many scholars the big data era) artificial intelligence (hereinafter AI) get more and more attention from the public and from the different branches of sciences as well. What previously was a mere science-fiction, now starts to become reality. AI and robotics often walk hand in hand, what changes not only the business and industrial life, but also has a serious impact on the legal system. The main research of the author focuses on these impacts in the field of private law, with special regards to liability and intellectual property issues. Many questions arise in these areas connecting to AI and robotics, where the boundaries are not sufficiently clear, and different needs are articulated by the different stakeholders. Recognizing the urgent need of thinking the Committee on Legal Affairs of the European Parliament adopted a Motion for a European Parliament Resolution A8-0005/2017 (of January 27th, 2017) in order to take some recommendations to the Commission on civil law rules on robotics and AI. This document defines some crucial usage of AI and/or robotics, e.g. the field of autonomous vehicles, the human job replacement in the industry or smart applications and machines. It aims to give recommendations to the safe and beneficial use of AI and robotics. However – as the document says – there are no legal provisions that specifically apply to robotics or AI in IP law, but that existing legal regimes and doctrines can be readily applied to robotics, although some aspects appear to call for specific consideration, calls on the Commission to support a horizontal and technologically neutral approach to intellectual property applicable to the various sectors in which robotics could be employed. AI can generate some content what worth copyright protection, but the question came up: who is the author, and the owner of copyright? The AI itself can’t be deemed author because it would mean that it is legally equal with the human persons. But there is the programmer who created the basic code of the AI, or the undertaking who sells the AI as a product, or the user who gives the inputs to the AI in order to create something new. Or AI generated contents are so far from humans, that there isn’t any human author, so these contents belong to public domain. The same questions could be asked connecting to patents. The research aims to answer these questions within the current legal framework and tries to enlighten future possibilities to adapt these frames to the socio-economical needs. In this part, the proper license agreements in the multilevel-chain from the programmer to the end-user become very important, because AI is an intellectual property in itself what creates further intellectual property. This could collide with data-protection and property rules as well. The problems are similar in the field of liability. We can use different existing forms of liability in the case when AI or AI led robotics cause damages, but it is unsure that the result complies with economical and developmental interests.

Keywords: artificial intelligence, intellectual property, liability, robotics

Procedia PDF Downloads 176

Authors: Kalin Ivanov, Stanislava Ivanova

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Actoprotectors are substances with hight performance enchasing potential and hight antioxidant activity. Most of these drugs have been developed in USSR for military medicine purposes. Based on their chemical composition actoprotectors could be classified into three categories: benzimidazole derivatives (ethomersol, bemitil); adamantane derivatives (bromantane), other chemical classes. First data for intake of actoprotectors from professional athletes is from 1980. The daily intake of actoprotectors demonstrate many benefits for athletes like: positive effect on the efficiency of physical work, antihypoxic effects, antioxidant effects, nootropic effects, rapid recovery. Since 1997, bromantane is considered as doping. This is a result of Summer Olympic Games in Athlanta (1996) when several Russian athletes tested positive for bramantane. Even the drug is safe for athletes health its use is considered as violation of anti- doping rules. More than 37 years bemetil has been used by professional athletes with no risk but currently it is included in WADA monitoring programme for 2018. Current perspectives are that most used actoprotectors would be considered as doping. Many clinical studies have confirmed that intake of bemitil and bromantan demonstrate positive influence on the physical work capacity but data for other actoprotectors like chlodantane, ademol, ethomersol is limited.

Keywords: actoprotector, sport, doping, bemitil

Procedia PDF Downloads 283

Authors: Jana Tchekalarova, Stela Georgieva, Petia Peneva, Petar Todorov

Abstract:

In the present study, a series of bioconjugates of N-modified hemorphine analogs containing second pharmacophore cinnamic acids (CA) or caffeic (KA) were synthesized by a traditional solid-phase Fmoc chemistry method for peptide synthesis. Electrochemical and fluorimetrical analysis and in vivo anticonvulsant activity in mice were conducted on the compounds. The three CA acids (H4-CA, H5-CA, and H7-CA) and three KA acids (H4-KA, H5-KA, and H7-KA)-conjugated hemorphine derivatives showed dose-dependent anticonvulsant activity in the maximal electroshock test (MES) in mice. The KA-conjugated H5-KA derivate was the only compound that suppressed clonic seizures at the lowest dose of 0.5 µg/mouse in the scPTZ test. The activity against the psychomotor seizures in the 6-Hz test was detected only for the H4-CA (0.5 µg) and H4-KA (0.5 µg and 1 µg), respectively. The peptide derivates did not exhibit neurotoxicity in the rotarod test. Our findings suggest that conjugated CA and KA hemorphine peptides can be used as a background for developing hemorphin-related analogs with anticonvulsant activity. Acknowledgements: This study is funded by the European Union-NextGenerationEU, through the National Recovery and Resilience Plan of the Republic of Bulgaria, project № BG-RRP-2.004-0002, "BiOrgaMCT".

Keywords: hemorphins, caffeic/cinnamic acid, anticonvulsant activity, electrochemistry, fluorimetry

Procedia PDF Downloads 66

Authors: Maryam Taheri, Mehdi Jahanfar, Kenji Ogino

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Fast drying traffic marking paint comprising a solvent-borne resin, a filler, a pigment and a solvent that is especially suitable for colder ambient (temperatures near freezing) applications, where waterborne traffic paint cannot be used. Acrylic resins based on methyl methacrylate, butyl acrylate, acrylic acid, and styrene were synthesized in different solvents using organic peroxide initiators such as peroxyester, peroxyketal, dialkylperoxide and azo. After polymerization, the molecular weight (Mw), polydispersity index= PDI (Mw/Mn), viscosity, total residual monomer and APHA color were evaluated and results of organic peroxide initiators (t- butyl and t-amyl derivatives) were also compared with the azo initiator. The Mw, PDI, viscosity, mass conversation and APHA color of resins with t-amyl derivatives of organic peroxide initiators are very proper. The results of the traffic marking paints test such as non-volatile matter, no- pick- up time, hiding power, resistance to wear and water resistance study that produced with these resins also confirm this.

Keywords: fast drying traffic marking paint, acrylic resin, organic peroxide initiator, peroxyester, peroxyketal, dialkylperoxide and azo initiator

Procedia PDF Downloads 177

Authors: Hetvi Trivedi

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Technological escalation cannot be negated. The same is true for the benefits of technology. However, such escalation has interfered with the traditional theories of protection under Intellectual Property Rights. Out of the many trends that have disrupted the old-school understanding of Intellectual Property Rights, one is hashtags. What began modestly in the year 2007 has now earned a remarkable status, and coupled with the unprecedented rise in social media the hashtag culture has witnessed a monstrous growth. A tiny symbol on the keypad of phones or computers is now a major trend which also serves companies as a critical investment measure in establishing their brand in the market. Due to this a section of the Intellectual Property Rights- Trademarks is undergoing a humungous transformation with hashtags like #icebucket, #tbt or #smilewithacoke, getting trademark protection. So, as the traditional theories of IP take on the modern trends, it is necessary to understand the change and challenge at a theoretical and proportional level and where need be, question the change. Traditionally, Intellectual Property Rights serves the societal need for intellectual productions that ensure its holistic development as well as cultural, economic, social and technological progress. In a two-pronged effort at ensuring continuity of creativity, IPRs recognize the investment of individual efforts that go into creation by way of offering protection. Commonly placed under two major theories- Utilitarian and Natural, IPRs aim to accord protection and recognition to an individual’s creation or invention which serve as an incentive for further creations or inventions, thus fully protecting the creative, inventive or commercial labour invested in the same. In return, the creator by lending the public the access to the creation reaps various benefits. This way Intellectual Property Rights form a ‘social contract’ between the author and society. IPRs are similarly attached to a social function, whereby individual rights must be weighed against competing rights and to the farthest limit possible, both sets of rights must be treated in a balanced manner. To put it differently, both the society and the creator must be put on an equal footing with neither party’s rights subservient to the other. A close look through doctrinal research, at the recent trend of trademark protection, makes the social function of IPRs seem to be moving far from the basic philosophy. Thus, where technology interferes with the philosophies of law, it is important to check and allow such growth only in moderation, for none is superior than the other. The human expansionist nature may need everything under the sky that can be tweaked slightly to be counted and protected as Intellectual Property- like a common parlance word transformed into a hashtag, however IP in order to survive on its philosophies needs to strike a balance. A unanimous global decision on the judicious use of IPR recognition and protection is the need of the hour.

Keywords: hashtag trademarks, intellectual property, social function, technology

Procedia PDF Downloads 101

Authors: Sara El Mansouria Beghdadi

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Quantitative structure–activity relationship (QSAR) modelling is one of the main computer tools used in medicinal chemistry. Over the past two decades, the incidence of fungal infections has increased due to the development of resistance. In this study, the QSAR was performed on a series of esters of 2-carboxamido-3-(1H-imidazole-1-yl) propanoic acid derivatives. These compounds have showed moderate and very good antifungal activity. The multiple linear regression (MLR) was used to generate the linear 2d-QSAR models. The dataset consists of 115 compounds with their antifungal activity (log MIC) against «Candida albicans» (ATCC SC5314). Descriptors were calculated, and different models were generated using Chemoffice, Avogadro, GaussView software. The selected model was validated. The study suggests that the increase in lipophilicity and the reduction in the electronic character of the substituent in R1, as well as the reduction in the steric hindrance of the substituent in R2 and its aromatic character, supporting the potentiation of the antifungal effect. The results of QSAR could help scientists to propose new compounds with higher antifungal activities intended for immunocompromised patients susceptible to multi-resistant nosocomial infections.

Keywords: quantitative structure–activity relationship, imidazole, antifungal, candida albicans (ATCC SC5314)

Procedia PDF Downloads 50

Authors: M. Koksal, T. Ozyazici, E. Gurdal, M. Yarım, E. Demirpolat, M. B. Y. Aycan

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The discovery of new drugs in cancer chemotherapy is still a major topic because of severe side effects, selectivity problems and resistance development potential of existing drugs. In recent years, combined anticancer therapies or multi-acting drugs are clinically preferred over traditional cytotoxic treatment, with the aim of avoiding resistance and toxic side effects. Arrangement of multi-acting targets can be carried out either by combination of several drugs with different mechanisms or by usage of a single chemical compound capable of regulating several targets of a disease with multiple factors. In literature, several pyrimidine and piperazine derivatives have been involved in the structure of many compounds which have been used as chemotherapeutic agents along with wide clinical applications. The aim of this study is to combine pyrimidine and piperazine core structures to research and develop novel piperazinylpyrimidine derivatives with selective cytotoxicity over cancer cells. In this study, a group of novel 6-fluorophenyl-3-[2-(substitutedpiperazinyl)ethyl] hexahydropyrimidine-2,4-dione derivatives designed to observe the desired anticancer activity due to pyrimidine and piperazine based scaffolds. Target compounds were obtained by the reaction of appropriate piperazine derivatives and 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione. The synthetic pathway of 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione was started with Rodionov reaction using aldehyde, malonic acid and ammonium acetate in ethanol. Isolated β-fluorophenyl-β-amino acids were treated with 2-chloroethylisocyanate in the presence of an aqueous sodium hydroxide solution at room temperature to yield the sodium salts of the corresponding ureido acids. By addition of a mineral acid, ureido acids were precipitated. Later, these ureido acids were refluxed in thionyl chloride to give the 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-di-one which were furthermore treated with secondary amines. Structures of purified compounds were characterized with IR, 1H-NMR, 13C-NMR, mass spectroscopies and elemental analysis. All of the compounds gave satisfactory analytical and spectroscopic data, which were in full accordance with their depicted structures. In IR spectra of the compounds, N-H group was seen at 3230-3213 cm⁻¹. C-H was seen at 3100-2820 cm⁻¹ and C=O vibrational peaks were observed approximately at 1725 and 1665 cm⁻¹ in accordance with literature. In the NMR spectra of target compounds, the methylene protons of piperazine give two separate multiplet peaks around 3.5 and 4.5 ppm representing the successful N-alkylation of the structure. The cytotoxic activity of the synthesized compounds was investigated on human bronchial epithelial (BEAS 2B), lung (A549), colon adenocarcinoma (COLO205) and breast (MCF7) cell lines, by means of sulphorhodamine B (SRB) assays in triplicate. IC₅₀ values of the screened derivatives were found in range of 11.8-78 µM. This project was supported by The Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 215S157).

Keywords: cytotoxicity, hexahydropyrimidine, piperazine, sulphorhodamine B assay

Procedia PDF Downloads 130

Authors: G. B. Lim, C. H. Jeon, K. H. Jung

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General light metal alloys are often developed in the material of transportation equipment such as automobiles and aircraft. Among the light metal alloys, magnesium is the lightest structural material with superior specific strength and many attractive physical and mechanical properties. However, magnesium alloys were difficult to obtain the mechanical properties at warm temperature. The aims of present work were to establish an analytical relation between mechanical properties and plastic flow induced by local indentation. An experimental investigation of the local strain distribution was carried out using a specially designed local indentation equipment in conjunction with ARAMIS based on digital image correlation method.

Keywords: indentation, magnesium, mechanical property, lightweight material, ARAMIS

Procedia PDF Downloads 451

Authors: Pierre Mintom, William Djeukeu Asongni, Michelle Moni, William Dakam, Christine Fernande Nyangono Biyegue.

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Background: In order to prevent congestive heart failure, control of hypertension and hypercholesterolemia is necessary because those risk factors frequently occur in combination. Objective: The aim of the study is to determine the prevalence and risk factors of hypertension, hypercholesterolemia and double burden HTA-Hypercholesterolemia in patients with congestive heart failure. Methodology: A database of 98 patients suffering from congestive heart failure was used. The latter were recruited from August 15, 2017, to March 5, 2018, in the Cardiology department of Deido District Hospital of Douala. This database provides information on sociodemographic parameters, biochemical examinations, characteristics of heart failure and food consumption. ESC/ESH and NCEP-ATPIII definitions were used to define Hypercholesterolemia (total cholesterol ≥200mg/dl), Hypertension (SBP≥140mmHg and/or DBP≥90mmHg). Double burden hypertension-hypercholesterolemia was defined as follows: total cholesterol (CT)≥200mg/dl, SBP≥140mmHg and DBP≥90mmHg. Results: The prevalence of hypertension (HTA), hypercholesterolemia (hyperchol) and double burden HTA-Hyperchol were 61.2%, 66.3% and 45.9%, respectively. No sociodemographic factor was associated with hypertension, hypercholesterolemia and double burden, but Male gender was significantly associated (p<0.05) with hypercholesterolemia. HypoHDLemia significantly increased hypercholesterolemia and the double burden by 19.664 times (p=0.001) and 14.968 times (p=0.021), respectively. Regarding dietary habits, the consumption of rice, peanuts and derivatives and cottonseed oil respectively significantly (p<0.05) exposed to the occurrence of hypertension. The consumption of tomatoes, green bananas, corn and derivatives, peanuts and derivatives and cottonseed oil significantly exposed (p<0.05) to the occurrence of hypercholesterolemia. The consumption of palm oil and cottonseed oil exposed the occurrence of the double burden of hypertension-hypercholesterolemia. Consumption of eggs protects against hypercholesterolemia, and consumption of peanuts and tomatoes protects against the double burden. Conclusion: hypercholesterolemia associated with hypertension appears as a complicating factor of congestive heart failure. Key risk factors are mainly diet-based, suggesting the importance of nutritional education for patients. New management protocols emphasizing diet should be considered.

Keywords: risk factors, hypertension, hypercholesterolemia, congestive heart failure

Procedia PDF Downloads 42

Authors: Burak Unveren, Ecem Uygun, Özdemi̇r Teke

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A large body of literature documents how the Ottoman Empire's economic decline in relation to Western Europe was exacerbated by the unequal legal treatment of its subjects based on creed. Motivated by this debate, we empirically explore whether property taxes collected from businesses in Istanbul discriminated against or favored non-Muslims after the cadastral survey of the capital in 1875. The survey was conducted to determine the property taxes. And the process was potentially susceptible to the biased views of the surveyors who calculated the taxes payable via their subjective appraisals of all real properties. According to our results, in contrast to widely held beliefs regarding 19th-century Istanbul, the number of Muslim shop owners is higher than that of non-Muslims. Moreover, we find evidence for taxes collected from non-Muslim shop and store owners to be higher compared to Muslims, even after controlling for all physical features (e.g., size, location, etc.). These results directly pertain to the fiscal capacity of the Ottoman state and its economic divergence from Europe in the 19th century. Surprisingly, the data also indicates no statistically different tax differentials between male and female property owners.

Keywords: economic history, taxation, small business, discrimination

Procedia PDF Downloads 41

Authors: S. Karklina, I. Erins

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The main problem is that there is a very low innovation performance in Latvia. Since Latvia is a Member State of European Union, it also shall have to fulfill the set targets and to improve innovative results. Universities are one of the main performers to provide innovative capacity of country. University, industry and government need to cooperate for getting best results. The intellectual property is one of the indicators to determine innovation level in the country or organization and patents are one of the characteristics of intellectual property. The objective of the article is to determine indicators characterizing innovative environment in Latvia and influence of the development of universities on them. The methods that will be used in the article to achieve the objectives are quantitative and qualitative analysis of the literature, statistical data analysis, and graphical analysis methods.

Keywords: HEI, innovations, Latvia, patents

Procedia PDF Downloads 290

Authors: Ozlem Temiz-Arpaci, Meryem Tasci, Fatma Sezer Senol, İlkay Erdogan Orhan

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Alzheimer’s disease (AD), a neurodegenerative disorder characterized by a progressive deterioration of memory and cognition, occurs more frequently in elderly people. Current treatment approaches in this disease with the major therapeutic strategy are based on the AChE and BChE inhibition. On the other hand, tyrosinase inhibition has become a target for the treatment of Parkinson’s disease (PD) since this enzyme may play a role in neuromelanin formation in the human brain and could be critical in the formation of dopamine neurotoxicity associated with neurodegeneration linked to PD. Also benzoxazoles are structural isosteres of natural nucleotides that can interact with biopolymers so that benzoxazoles showed a lot of different biological activities. In this study, a series of 2,5-disubstituted-benzoxazole derivatives were synthesized and were evaluated as possible inhibitors of acetylcholinesterase (AChE) / butyrylcholinesterase (BChE) and tyrosinase. The results demonstrated that the compounds exhibited a weak spectrum of AChE / BChE inhibitory activity ranging between 3.92% - 54.32% except compound 8 which showed no activity against AChE and compound 4 which showed no activity against BChE at the specified molar concentrations. Also, the compounds indicated lower than tyrosinase inhibitory activity of ranging between 8.14% - 22.90% to that of reference (kojic acid).

Keywords: AChE and BChE inhibition, Alzheimer’s disease, benzoxazoles, tyrosinase inhibition

Procedia PDF Downloads 311

Authors: Payel Ghosh, Rama Chandra Pradhan, Sabyasachi Mishra

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Jamun (Syzygium cuminii L.) is one of the important indigenous minor fruit with high medicinal value. The jamun cultivation is unorganized and there is huge loss of this fruit every year. The perishable nature of the fruit makes its postharvest management further difficult. Due to the strong cell wall structure of pectin-protein bonds and hard seeds, extraction of juice becomes difficult. Enzymatic treatment has been commercially used for improvement of juice quality with high yield. The objective of the study was to optimize the best treatment method for juice extraction. Enzymes (Pectinase and Tannase) from different stains had been used and for each enzyme, best result obtained by using response surface methodology. Optimization had been done on the basis of physicochemical property, nutritional property, sensory quality and cost estimation. According to quality aspect, cost analysis and sensory evaluation, the optimizing enzymatic treatment was obtained by Pectinase from Aspergillus aculeatus strain. The optimum condition for the treatment was 44 ^oC with 80 minute with a concentration of 0.05% (w/w). At these conditions, 75% of yield with turbidity of 32.21NTU, clarity of 74.39%T, polyphenol content of 115.31 mg GAE/g, protein content of 102.43 mg/g have been obtained with a significant difference in overall acceptability.

Keywords: enzymatic treatment, Jamun, optimization, physicochemical property, sensory analysis

Procedia PDF Downloads 274

Authors: Umar Yusuf Batsari

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Let E be a uniformly smooth and uniformly convex real Banach space and C be a nonempty, closed and convex subset of E. Let $V= \{S_i : C\to C, ~i=1, 2, 3\cdots N\}$ be a convex set of relatively nonexpansive mappings containing identity. In this paper, an iterative sequence obtained from CQ algorithm was shown to have strongly converge to a point $\hat{x}$ which is a common fixed point of relatively nonexpansive mappings in V and also solve the system of equilibrium problems in E. The result improve some existing results in the literature.

Keywords: relatively nonexpansive mappings, strong convergence, equilibrium problems, uniformly smooth space, uniformly convex space, convex set, kadec klee property

Procedia PDF Downloads 394

Authors: Lana Horvat Dmitrović

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The main purpose of this paper is to study the box dimension as fractal property of bifurcations of discrete dynamical systems in higher dimensions. The paper contains the fractal analysis of the orbits near the hyperbolic and non-hyperbolic fixed points in discrete dynamical systems. It is already known that in one-dimensional case the orbit near the hyperbolic fixed point has the box dimension equal to zero. On the other hand, the orbit near the non-hyperbolic fixed point has strictly positive box dimension which is connected to the non-degeneracy condition of certain bifurcation. One of the main results in this paper is the generalisation of results about box dimension near the hyperbolic and non-hyperbolic fixed points to higher dimensions. In the process of determining box dimension, the restriction of systems to stable, unstable and center manifolds, Lipschitz property of box dimension and the notion of projective box dimension are used. The analysis of the bifurcations in higher dimensions with one multiplier on the unit circle is done by using the normal forms on one-dimensional center manifolds. This specific change in box dimension of an orbit at the moment of bifurcation has already been explored for some bifurcations in one and two dimensions. It was shown that specific values of box dimension are connected to appropriate bifurcations such as fold, flip, cusp or Neimark-Sacker bifurcation. This paper further explores this connection of box dimension as fractal property to some specific bifurcations in higher dimensions, such as fold-flip and flip-Neimark-Sacker. Furthermore, the application of the results to the unit time map of continuous dynamical system near hyperbolic and non-hyperbolic singularities is presented. In that way, box dimensions which are specific for certain bifurcations of continuous systems can be obtained. The approach to bifurcation analysis by using the box dimension as specific fractal property of orbits can lead to better understanding of bifurcation phenomenon. It could also be useful in detecting the existence or nonexistence of bifurcations of discrete and continuous dynamical systems.

Keywords: bifurcation, box dimension, invariant manifold, orbit near fixed point

Procedia PDF Downloads 223

Authors: Neda Lovričević, Đilda Pečarić, Josip Pečarić

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The Jensen functional in its discrete form is brought in relation to the Csiszar divergence functional, this time via its monotonicity property. This approach presents a generalization of the previously obtained results that made use of interpolating Jensen-type inequalities. Thus the monotonicity property is integrated with the Zipf-Mandelbrot law and applied to f-divergences for probability distributions that originate from the Csiszar divergence functional: Kullback-Leibler divergence, Hellinger distance, Bhattacharyya distance, chi-square divergence, total variation distance. The Zipf-Mandelbrot and the Zipf law are widely used in various scientific fields and interdisciplinary and here the focus is on the aspect of the mathematical inequalities.

Keywords: Jensen functional, monotonicity, Csiszar divergence functional, f-divergences, Zipf-Mandelbrot law

Procedia PDF Downloads 113

Authors: Peng Cheng, Liqing Wei, Hongyu Chen, Ruomiao Wang

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This paper discusses a light-weight reinforced thermoplastic (LWRT) composite with superior fire retardancy. This porous LWRT composite is manufactured using polyolefin, fiberglass, and fire retardant additives via a wet-lay process. However, discoloration of the LWRT can be induced by various mechanisms, which may be a concern in the building and construction industry. It is commonly understood that discoloration is strongly associated with the presence of phenolic antioxidant(s) and NO_x. The over-oxidation of phenolic antioxidant(s) is probably the root-cause of the discoloration (pinking/yellowing). Hanwha Azdel, Inc. developed a LWRT with fire-retardant property of ASTM E84-Class A specification, as well as negligible discoloration even under harsh conditions. In addition, this thermoplastic material is suitable for secondary processing (e.g. compression molding) if necessary.

Keywords: discoloration, fire-retardant, thermoplastic composites, wet-lay process

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Authors: Manasi Roy, Raju Mondal

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During last two decades the synthesis and design of MOFs or novel coordination polymers (CPs) has flourished as an emerging area of research due to their role as functional materials. Accordingly, ten new cobalt-based MOFs have been synthesized using a simple bispyrazole ligand, 4,4′-methylene-bispyrazole (H2MBP), and isophthalic acid (H2IPA) and its four 5-substituted derivatives R-H2IPA (R = COOH, OH, tBu, NH2). The major aim of this study was to validate the mutual influence of temperature and substitutions on the final structural self-assembly. Five different isophthalic acid derivatives were used to study the influence of substituents while each reaction was carried out at two different temperatures to assess the temperature effect. A clear correlation was observed between the reaction temperature and the coordination number of the cobalt atoms which consequently changes the self assembly pattern. Another fact that the periodical change in coordination number did bring about some systematic changes in the structural network via secondary building unit selectivity. With the presence of a tunable cavity inside the network, and unsaturated metal centers, MOFs show highly encouraging photocatalytic degradation of toxic dye with a potential application in waste water purification. Another fascinating aspect of this work is the construction of magnetic coordination polymers with the occurrence of a not-so-common MCE behavior of cobalt-based MOF.

Keywords: MOFs, temperature effect, MCE, dye degradation

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Authors: Elena Ionescu, Elena Iacob, Marie-Louise Ionescu, Carmen Elena Tebrencu, Oana Teodora Ciuperca

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Echinacea species (Asteraceae) has received a global attention because it is widely used for treatment of cold, flu and upper respiratory tract infections. Echinacea species contain a great variety of chemical components that contribute to their activity. The most important components responsible for the biological activity are those with high molecular-weight such as polysaccharides, polyacetylenes, highly unsaturated alkamides and caffeic acid derivatives. The principal factors that may influence the chemical composition of Echinacea include the species and the part of plant used (aerial parts or roots ). In recent years the market for Echinacea has grown rapidly and also the cases of adultery/replacement especially for Echinacea root. The identification of presence or absence of same biomarkers provide information for safe use of Echinacea species in food supplements industry. The aim of the study was the preliminary evaluation and fingerprinting by UV-VISIBLE spectroscopy of biomarkers in terms of content in phenolic derivatives of some Echinacea species (E. purpurea, E. angustifolia and E. pallida) for identification and authentication of the species. The steps of the study were: (1) samples (extracts) preparation from Echinacea species (non-hydrolyzed and hydrolyzed ethanol extracts); (2) samples preparation of reference substances (polyphenol acids: caftaric acid, caffeic acid, chlorogenic acid, ferulic acid; flavonoids: rutoside, hyperoside, isoquercitrin and their aglycones: quercitri, quercetol, luteolin, kaempferol and apigenin); (3) identification of specific absorption at wavelengths between 700-200 nm; (4) identify the phenolic compounds from Echinacea species based on spectral characteristics and the specific absorption; each class of compounds corresponds to a maximum absorption in the UV spectrum. The phytochemical compounds were identified at specific wavelengths between 700-200 nm. The absorption intensities were measured. The obtained results proved that ethanolic extract showed absorption peaks attributed to: phenolic compounds (free phenolic acids and phenolic acids derivatives) registrated between 220-280 nm, unsymmetrical chemical structure compounds (caffeic acid, chlorogenic acid, ferulic acid) with maximum absorption peak and absorption "shoulder" that may be due to substitution of hydroxyl or methoxy group, flavonoid compounds (in free form or glycosides) between 330-360 nm, due to the double bond in position 2,3 and carbonyl group in position 4 flavonols. UV spectra showed two major peaks of absorption (quercetin glycoside, rutin, etc.). The results obtained by UV-VIS spectroscopy has revealed the presence of phenolic derivatives such as cicoric acid (240 nm), caftaric acid (329 nm), caffeic acid (240 nm), rutoside (205 nm), quercetin (255 nm), luteolin (235 nm) in all three species of Echinacea. The echinacoside is absent. This profile mentioned above and the absence of phenolic compound echinacoside leads to the conclusion that species harvested as Echinacea angustifolia and Echinacea pallida are Echinacea purpurea also; It can be said that preliminary fingerprinting of Echinacea species through correspondence with the phenolic derivatives profile can be achieved by UV-VIS spectroscopic investigation, which is an adequate technique for preliminary identification and authentication of Echinacea in medicinal herbs.

Keywords: Echinacea species, Fingerprinting, Phenolic compounds, UV-VIS spectroscopy

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Authors: Periklis Brakatsoulas

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Recent empirical research shows a growing interest in investment decision-making under market anomalies that contradict the rational paradigm. Momentum is undoubtedly one of the most robust anomalies in the empirical asset pricing research and remains surprisingly lucrative ever since first documented. Although predominantly phenomena identified across equities, momentum premia are now evident across various asset classes. Yet few many attempts are made so far to provide traders a diversified portfolio of strategies across different assets and markets. Moreover, literature focuses on patterns from past returns rather than mechanisms to signal future price directions prior to momentum runs. The aim of this paper is to develop a diversified portfolio approach to price distortion signals using daily position data on stocks, credit derivatives, and bonds. An algorithm allocates assets periodically, and new investment tactics take over upon price momentum signals and across different ranking groups. We focus on momentum life cycles, trend reversals, and price acceleration signals. The main effort here concentrates on the density, time span and maturity of momentum phenomena to identify consistent patterns over time and measure the predictive power of buy-sell signals generated by these anomalies. To tackle this, we propose a two-stage modelling process. First, we generate forecasts on core macroeconomic drivers. Secondly, satellite models generate market risk forecasts using the core driver projections generated at the first stage as input. Moreover, using a combination of the ARFIMA and FIGARCH models, we examine the dependence of consecutive observations across time and portfolio assets since long memory behavior in volatilities of one market appears to trigger persistent volatility patterns across other markets. We believe that this is the first work that employs evidence of volatility transmissions among derivatives, equities, and bonds to identify momentum life cycle patterns.

Keywords: forecasting, long memory, momentum, returns

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Authors: Abdulrahman Fahim M. Alsulami

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The current research seeks to explore the regulation of vaccine-related IP rights in light of the areas of divergence between the Trade-Related Aspects of Intellectual Property Rights (TRIPS) Agreement and investment treaties. The study is conducted in the context of the COVID-19 pandemic; therefore, it seems natural that a specific chapter is devoted to the examination of vaccine arrangements related to vaccine supplies. The chapter starts with the examination of a typical vaccine from the perspective of IP rights. It presents the distinctive features of vaccines as pharmaceutical products and investments, reviews the basics of their patent protection, reviews vaccines’ components, and discusses IPR protection of different components of vaccines. The subsection that focuses on vaccine development and licensing reviews vaccine development stages investigates differences between vaccine licensing in different countries and presents barriers to vaccine licensing. The third subsection, at the same time, introduces the existing arrangements related to COVID-19 vaccine supplies, including COVAX arrangements, international organizations’ assistance, and direct negotiations between governments and vaccine manufacturers.

Keywords: bilateral investment treaties, COVID-19 vaccine, IP rights, TRIPs agreement

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Authors: Jyoti Singh, Ranju Bansal

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Fighting pain and inflammation is a common problem faced by physicians while dealing with a wide variety of diseases. Since ancient time nonsteroidal anti-inflammatory agents (NSAIDs) and opioids have been the cornerstone of treatment therapy, however, the usefulness of both these classes is limited due to severe side effects. NSAIDs, which are mainly used to treat mild to moderate inflammatory pain, induce gastric irritation and nephrotoxicity whereas opioids show an array of adverse reactions such as respiratory depression, sedation, and constipation. Moreover, repeated administration of these drugs induces tolerance to the analgesic effects and physical dependence. Further discovery of selective COX-2 inhibitors (coxibs) suggested safety without any ulcerogenic side effects; however, long-term use of these drugs resulted in kidney and hepatic toxicity along with an increased risk of secondary cardiovascular effects. The basic approaches towards inflammation and pain treatment are constantly changing, and researchers are continuously trying to develop safer and effective anti-inflammatory drug candidates for the treatment of different inflammatory conditions such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, psoriasis and multiple sclerosis. Synthetic 3(2H)-pyridazinones constitute an important scaffold for drug discovery. Structure-activity relationship studies on pyridazinones have shown that attachment of a lactam at N-2 of the pyridazinone ring through a methylene spacer results in significantly increased anti-inflammatory and analgesic properties of the derivatives. Further introduction of the heterocyclic ring at lactam nitrogen results in improvement of biological activities. Keeping in mind these SAR studies, a new series of compounds were synthesized as shown in scheme 1 and investigated for anti-inflammatory, analgesic, anti-platelet activities and docking studies. The structures of newly synthesized compounds have been established by various spectroscopic techniques. All the synthesized pyridazinone derivatives exhibited potent anti-inflammatory and analgesic activity. Homoveratryl substituted derivative was found to possess highest anti-inflammatory and analgesic activity displaying 73.60 % inhibition of edema at 40 mg/kg with no ulcerogenic activity when compared to standard drugs indomethacin. Moreover, 2-substituted-4-benzo[d][1,3]dioxole-6-phenylpyridazin-3(2H)-ones derivatives did not produce significant changes in bleeding time and emerged as safe agents. Molecular docking studies also illustrated good binding interactions at the active site of the cyclooxygenase-2 (hCox-2) enzyme.

Keywords: anti-inflammatory, analgesic, pyridazin-3(2H)-one, selective COX-2 inhibitors

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Authors: Yongkui Cui, Fengping Wang, Hailei Zhao, Muhammad Zubair Iqbal, Ziya Wang, Yan Li, Pengpeng LV

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The novel 3D SnO cabbages self-assembled by nanosheets were successfully synthesized via template-free hydrothermal growth method under facile conditions.The XRD results manifest that the as-prepared SnO is tetragonal phase. The TEM and HRTEM results show that the cabbage nanosheets are polycrystalline structure consisted of considerable single-crystalline nanoparticles. Two typical Raman modes A1g=210 and Eg=112 cm-1 of SnO are observed by Raman spectroscopy. Moreover, galvanostatic cycling tests has been performed using the SnO cabbages as anode material of lithium ion battery and the electrochemical results suggest that the synthesized SnO cabbage structures are a promising anode material for lithium ion batteries.

Keywords: electrochemical property, hydrothermal synthesis, lithium ion battery, stannous oxide

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Authors: Islem Kedidi, Rihab Bedoui Bensalem, Faysal Manssouri

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In traditional models of insurance data, the number and size of claims are assumed to be independent. Relaxing the independence assumption, this article explores the Vine copula to model dependence structure between multivariate frequency and average severity of insurance claim. To illustrate this approach, we use the Wisconsin local government property insurance fund which offers several insurance protections for motor vehicles, property and contractor’s equipment claims. Results show that the C-vine copula can better characterize the multivariate dependence structure between frequency and severity. Furthermore, we find significant dependencies especially between frequency and average severity among different coverage types.

Keywords: dependency modeling, government insurance, insurance claims, vine copula

Procedia PDF Downloads 172

Authors: Jia H. Wong, Jingli Zhang, Habsah Mohamad, Iswatun H. Abdullah Ripain, Muhammad Bilal, Amelia J. Lloyd, Abdul A. Mohamed Yusoff, Jafri M. Abdullah

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Epilepsy is one of the most common neurological diseases affecting more than 50 million of people worldwide. Epilepsy is a state of recurrent, spontaneous seizures with multiple syndromes and symptoms of different causes of brain dysfunction, prognosis, and treatments; characterized by transient, occasional and stereotyped interruptions of behavior whereby the excitatory-inhibitory activities within the central nervous system (CNS) are thrown out of balance due to various kinds of interferences. The goal of antiepileptic treatment is to enable patients to be free from seizures or to achieve control of seizures through surgical treatment and/or pharmacotherapy. Pharmacotherapy through AED plays an important role especially in countries with epilepsy treatment gap due to costs and availability of health facilities, skills and resources, yet there are about one-third of the people with epilepsy have drug-resistant seizures. Hence, this poses considerable challenges to the healthcare system and the effort in providing cost-effective treatment as well as the search for alternatives to treatment and management of epilepsy. Enhancement of γ-aminobutyric acid (GABA)-mediated inhibitory neurotransmission is one of the key mechanisms of actions of antiepileptic drugs. GABA type > a receptors (GABAAR) are ligand-gated ion channels that mediate rapid inhibitory neurotransmission upon the binding of GABA with a heteropentameric structure forming a central pore that is permeable to the influx of chloride ions in its activated state. The major isoform of GABAA receptors consists of two α1, two β2, and one γ2 subunit. It is the most abundantly expressed combinations in the brain and the most commonly researched through Xenopus laevis oocytes. With the advancing studies on ethnomedicine and traditional treatments using medicinal plants, increasing evidence reveal that spice and herb plants with medicinal properties play an important role in the treatment of ailments within communities across different cultures. Capsaicin is the primary natural capsaicinoid in hot peppers of plant genus Capsicum, consist of an aromatic ring, an amide linkage and a hydrophobic side chain. The study showed that capsaicins conferred neuroprotection in status epilepticus mouse models through anti-ictogenic, hypothermic, antioxidative, anti-inflammatory, and anti-apoptotic actions in a dose-dependent manner. In this study, five capsaicin derivatives were tested for their ability to increase the GABA-induced chloride current on α1β2γ2S of GABAAR expressed on Xenopus laevis oocytes using the method of two-microelectrode voltage clamp. Two of the capsaicin derivatives, IS5 (N-(4-hydroxy-3-methoxybenzyl)-3-methylbutyramide) and IS10 (N-(4-hydroxy-3-methoxybenzyl)-decanamide) at a concentration of 30µM were able to significantly increase the GABA-induced chloride current with p=0.002 and p=0.026 respectively. This study were able to show the enhancement effect of two capsaicin derivatives with moderate length of hydrocarbon chain on this receptor subtype, revealing the promising inhibitory activity of capsaicin derivatives through enhancement of GABA-induced chloride current and further investigations should be carried out to verify its antiepileptic effects in animal models.

Keywords: α1β2γ2 GABAA receptors, α1β2γ2S, antiepileptic, capsaicin derivatives, two-microelectrode voltage clamp, Xenopus laevis oocytes

Procedia PDF Downloads 335