Search results for: benzyl isothiocyanate

Authors: Espinoza S. Clara, Gamarra Q. Flor, Marianela F. Ramos Quispe S. Miguel, Flores R. Omar

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Tropaeolum majus L. is a native plant to South and Central America, used since ancient times by our ancestors to combat different diseases. Glucotropaeolonin is one of its main components, which when hydrolyzed, forms benzyl isothiocyanate (BIT) that promotes cellular apoptosis (programmed cell death in cancer cells). Therefore, the present research aims to evaluate the effect of the pressure and temperature of BIT extraction by supercritical CO₂ from Tropaeolum majus L. The extraction was carried out in a supercritical fluid extractor equipment Speed SFE BASIC Brand: Poly science, the leaves of Tropaeolum majus L. were ground for one hour and lyophilized until obtaining a humidity of 6%. The extraction with supercritical CO₂ was carried out with pressures of 200 bar and 300 bar, temperatures of 50°C, 60°C and 70°C, obtained by the conjugation of these six treatments. BIT was identified by thin layer chromatography using 98% BIT as the standard, and as the mobile phase hexane: dichloromethane (4:2). Subsequently, BIT quantification was performed by high performance liquid chromatography (HPLC). The highest yield of oleoresin by supercritical CO₂ extraction was obtained pressure 300 bar and temperature at 60°C; and the higher content of BIT at pressure 200 bar and 70°C for 30 minutes to obtain 113.615 ± 0.03 mg BIT/100 g dry matter was obtained.

Keywords: solvent extraction, Tropaeolum majus L., supercritical fluids, benzyl isothiocyanate

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Authors: Noreen Sajjad Ghulam Hussain

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Catalysts are prepared by simple physical mixing and thermal treatment of support and metal acetate precursors.The effect of metal ratio and metal loading to produce highly active catalyst for the oxidation of benzyl alcohol are studied.

Keywords: catalyst, acetates, benzyl alcohols

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Authors: Abdel Ghany F. Shoair, Mai M. A. H. Shanab

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The basic aqueous systems NiSO4.6H₂O / K₂S₂O₈ (PH= 14) or NiSO₄.6H₂O / KBrO₃ (PH = 11.5) were ‎investigated ‎for the ‎catalytic conversion benzyl alcohol and ‎some para-substituted benzyl ‎alcohols to their ‎corresponding ‎acids in 75-97 % yield at room ‎temperature. The active species ‎was isolated and characterized by scanning ‎electron ‎microscopy (SEM), ‎‎transmission electron microscopy (TEM), X-ray ‎powder diffraction, EDX and ‎‎FT-IR ‎techniques and identified as NiO₂ nanoparticles (NPNPs). The SEM and ‎TEM images of nickel peroxide samples show a fine spherical-like ‎aggregation of ‎NiO₂ molecules with a nearly homogeneous partial size and confirm the ‎aggregation's size ‎to ‎be in the range of 2-3 nm. The yields, turnover (TO) and turn ‎over frequencies (TOF) were calculated. ‎It was noticed ‎that the aromatic alcohols ‎containing para-substituted electron donation groups gave better ‎‎yields than ‎those having electron-withdrawing groups. The optimum conditions for this ‎‎catalytic reaction ‎were studied using benzyl alcohol as a model. The mechanism ‎of the ‎catalytic conversion reaction was ‎suggested, in which the produced ‎(NPNPs) convert alcohols ‎to acids in two steps through the formation of the ‎‎corresponding aldehyde. The produced ‎NiO, because of this conversion, is ‎converted again to (NPNPs) by ‎an excess of K₂S₂O₈ or KBrO₃. This ‎catalytic cycle continues ‎until all the substrate is oxidized.

Keywords: Nickel, oxidation, catalysts, benzyl alcohol

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Authors: Tomasz Frączek, Agata Paneth, Rafał Kamiński, Agnieszka Krakowiak, Piotr Paneth

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Azoles are a promising class of the new generation of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs). From thousands of reported compounds, many possess the same basic structure of an aryl substituted azole ring linked by a thioglycolamide chain with another aromatic ring. To find novel extensions for this primary scaffold, we explored the 5-position substitution of triazole NNRTIs using molecular docking followed by synthesis of selected compounds. We discovered that heterocyclic substituents in 5-position of the triazole ring are detrimental to the inhibitory activity of compounds with 4-membered thioglycolamide linker. This substitution seems to be viable only for compounds with a shorter 2-membered linker such as in derivatives of 4‐benzyl‐3‐(benzyl-sulfanyl)‐5‐(thiophen‐2‐yl)‐4H‐1,2,4‐triazole reported earlier. A new scaffold of 2‐[(4‐benzyl‐5‐methyl‐4H‐1,2,4‐triazol‐3‐yl)sulfanyl]‐N‐phenylacetamide has been identified in this study.

Keywords: docking, molecular modeling, drug design, novel scaffolds

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Authors: Muhammad A. Muhammad

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Butenafine (N-4-tert-butyl benzyl-N-methyl-1-naphthylene methylamine hydrochloride) is a benzylamine antimycotic (antifungal) agent that has a broad spectrum of action. The quest for improved antimycotic action brought about many research on the structure-activity properties of butenafine in relation to other antifungal agents. Of all those research, only little or no effort was recorded on the substituents attached to the aromatic systems in butenafine. In this research, N-(4-(tert-butyl) benzyl)-1-(4-tert-butyl) phenyl)-N-methyl methanaminium chloride, which is a butenafine analogue was synthesised from tert-butyl benzyl derivatives, by reductive amination using various solvents through a direct approach, where 1,2-dichloroethane gave the best solvent action at 40 °C (Yield: 75%) and of all the reducing agents used, sodium borohydride was found to give the best reducing action in the presence of silica chloride at room temperature (Yield: 50%). Characterization of the compound by 1H NMR showed a singlet peak of 18 hydrogen atoms with a chemical shift at 1.3-1.5 ppm for the presence of 6 methyl groups in the two tert-butyl substituents, the 13C NMR also indicated the presence of the two tert-butyl substituents by the peak with a chemical shift at 31-32 ppm for the six methyl carbon atoms, the IR indicated the presence of a tertiary ammonium ion by a strong band at 2460 cm-1 and finally the EIS-MS confirmed the molar mass of the compound by a mass to charge ratio of 324.2693. These results suggested that the target molecule was actually synthesised and therefore, 1,2-dichloroethane is a good solvent for this synthesis, and the most suitable reducing agent is sodium borohydride.

Keywords: antimicrobial agents, antimycotic agents, butenafine, chemotherapeutic agents, semisynthetic agents

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Authors: Pankaj Dinesh Baviskar

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This study examines the impact of curcumin-loaded nano-spheres in the form of emulsions on fish eye cataracts. Curcumin nanoemulsions were prepared by using phenethyl isothiocyanate. Nanoemulsions were synthesized by ultrasound-assisted method at 150 Watt. A zeta potential measurement for curcumin-loaded nanoemulsions was found to be -30.7eV, -13.4eV, and -9.55eV, and particle size was found to be 149.3 nm, 245.3 and nm 403.5 nm using particle size analyzer respectively for different conditions. The surface morphology of nano-spheres was examined by FE-SEM analysis. The zeta potential measured indicates its stability for corresponding nano-spheres. The anti-cataract application was studied by using isolated fish eye lenses. The cataract was induced using high glucose concentrated solution. The biochemical parameters in the form of reduced glutathione were measured to interpret the anti-cataract ability of curcumin-loaded nanoemulsions.

Keywords: curcumin, nano, cataract, nanoemulsion

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Authors: V. Yurina, H. Sujuti, E. Rahmani, A. R. Nopitasari

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Breast cancer has the highest prevalence cancer in women. Moringa leaves (M. oleifera) contain quercetin, kaempferol, and benzyl isothiocyanate which can enhance induction of apoptosis. This research aimed to study the role of the leaf extract of Moringa to increase apoptosis in breast cancer cell line, MCF-7 cells. This research used in vitro experimental, post-test only, control group design on breast cancer cells MCF-7 in vitro. Moringa leaves were extracted by maceration method with ethanol 70%. Cells were treated with drumstick leaves extract on 1100, 2200, and 4400 μg/ml for Hsp27 and caspase-9 expression (immunocytochemistry) and apoptosis (TUNEL assay) test. The results of this study found that the IC50 2200 µg/ml. Moringa leaves extract can significantly increase the expression of caspase-9 (p<0.05) and decreased Hsp 27 expression (p<0.05). Moreover it can increase apoptosis (p<0.05) significantly in MCF-7 cells. The conclusion of this study is Moringa leaves extract is able to increase the expression of caspase-9, decrease Hsp27 expression and increase apoptosis in breast cancer cell-line MCF-7.

Keywords: apoptosis, breast cancer, caspase-9, Hsp27, Moringa oleifera

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Authors: M. S. M. Yusof, R. Ramli, S. K. C. Soh, N. Ismail, N. Ngah

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This study presents the synthesis of a series of methoxybenzoylthiourea amino acid derivatives. The compounds were obtained from the reactions between 2/3/4-methoxybenzoyl isothiocyanate with threonine. All of the compounds were characterized via mass spectrometry, ¹H and ¹³C NMR spectrometry, UV-Vis spectrophotometer and FT-IR spectroscopy. Mass spectra for all of the compounds showed the presence of molecular ion [M]⁺ peaks at m/z 312, which are in agreement to the calculated molecular weight. For ¹H NMR spectra, the presence of OCH₃, C=S-NH and C=O-NH protons were observed within range of δ_H 3.8-4.0 ppm, 11.1-11.5 ppm and 10.0-11.5 ppm, respectively. ¹³C NMR spectra in all compounds displayed the presence of OCH₃, C=O-NH, C=O-OH and C=S carbon resonances within range of δ_C 55.0-57.0 ppm, 165.0-168.0 ppm, 170.0-171.0 ppm and 180.0-182.0 ppm, respectively. In UV spectra, two absorption bands have been observed and both were assigned to the n-π* and π-π* transitions. Six vibrational modes of v(N-H), v(O-H), v(C=O-OH), v(C=O-NH), v(C=C) aromatic and v(C=S) appeared in the FT-IR spectra within the range of 3241-3467 cm^-1, 2976-3302 cm^-1, 1720-1768 cm^-1, 1655-1672 cm^-1, 1519-1525 cm^-1 and 754-763 cm^-1, respectively. The antibacterial activity for all of the compounds was screened against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium and Escherichia coli. However, no activity was observed.

Keywords: methoxybenzoyl isothiocyanate, amino acid, threonine, antibacterial

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Authors: S. K. Mohapatra, K. Ramanujam, S. Sankararaman

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Redox flow battery (RFB) is a preferred energy storage option for grid stabilisation and energy arbitrage as it offers energy and power decoupling. In contrast to aqueous RFBs (ARFBs), nonaqueous RFBs (NARFBs) could offer high energy densities due to the wider electrochemical window of the solvents used, which could handle high and low voltage organic redox couples without undergoing electrolysis. In this study, a RFB based on benzyl viologen hexafluorophosphate [BV(PF6)2] as anolyte and N-hexyl phenothiazine [HPT] as catholyte demonstrated. A cell operated with mixed electrolyte (1:1) containing 0.2 M [BV(PF₆)₂] and 0.2 M [HPT] delivered a coulombic efficiency (CE) of 95.3 % and energy efficiency (EE) 53%, with nearly 68.9% material utilisation at 40 mA cm-2 current density.

Keywords: non-aqueous redox flow battery, benzyl viologen, N-hexyl phenothiazine, mixed electrolyte

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Authors: Hasan Basri Jumin

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Application of crude palm oil waste combined to suitable concentration of benzyl-adenine give the significant effect to mean relative growth rate of vegetable plants and the same pattern in net assimilation rate crude palm oil waste has also significantly increased during 28 days old plants. Combination of treatment of suitable concentration of crude palm oil and benzyl adenine increased the growth and production of vegetable plants. The relative growth rate of vegetable plants was rapid 3 weeks after planting and gradually decreased at the end of the harvest time period. Combination of 400 mg.l-1 CPO with 1.0 mgl-1 till 10mgl-1 BA increased the Mean Relative Growth Rate (MRGR), Net assimilation rate (NAR), Leaf area and dry weight of Brassica juncea, Brassica oleraceae and Lactuca sativa.

Keywords: benzyladenine, crude-palm-oil, nutrient, vegetable, waste

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Authors: Seema Kothari, Dinesh Panday

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An observed correlation of the reaction rates with the changes in the nature of substituent present on one of the reactants often reveals the nature of transition state. Selective oxidation of organic compounds under non-aqueous media is an important transformation in synthetic organic chemistry. Inorganic chromates and dichromates being drastic oxidant and are generally insoluble in most organic solvents, a number of different chromium (VI) derivatives have been synthesized. Benzimidazolium dichromate (BIDC) is one of the recently reported Cr(VI) reagents which is neither hygroscopic nor light sensitive being, therefore, much stable. Not many reports on the kinetics of the oxidations by BIDC are seemed to be available in the literature. In the present investigation, the kinetics and mechanism of benzyl alcohol (BA) and a number of para- and meta-substituted benzyl alcohols by benzimidazolium dichromate (BIDC), in dimethyl sulphoxide, is reported. The reactions were followed spectrophotometrically at 364 nm by monitoring the decrease in [BIDC] for up to 85-90% reaction, the temperature being constant. The observed oxidation product is the corresponding benzaldehyde. The reactions were of first order with respect to each the alcohol and BIDC. The reactions are catalyzed by proton, and the dependence is of the form: kobs = a + b[H+]. The reactions thus follow both, an acid-dependent and acid-independent paths. The oxidation of [1,1 2H2]benzyl alcohol exhibited the presence of a substantial kinetic isotope effect ( kH/kD = 6.20 at 298 K ). This indicated the cleavage of a α-C-H bond in the rate-determining step. An analysis of the temperature dependence of the deuterium isotope effect showed that the loss of hydrogen proceeds through a concerted cyclic process. The rate of oxidation of BA was determined in 19 organic solvents. An analysis of the solvent effect by Swain’s equation indicated that though both the anion and cation-solvating powers of the solvent contribute to the observed solvent effect, the role of cation-solvation is major. The rates of the para and meta compounds, at 298 K, failed to exhibit a significant correlation in terms of Hammett or Brown's substituent constants. The rates were then subjected to analyses in terms of dual substituent parameter (DSP) equations. The rates of oxidation of the para-substituted benzyl alcohols show an excellent correlation with Taft's σI and σRBA values. However, the rates for the meta-substituted benzyl alcohols show an excellent correlation with σI and σR0. The polar reaction constants are negative indicating an electron-deficient transition state. Hence the overall mechanism is proposed to involve the formation of a chromate ester in a fast pre-equilibrium and then a decomposition of the ester in a subsequent slow step via a cyclic concerted symmetrical transition state, involving hydride-ion transfer, leading to the product. The first order dependence on alcohol may be accounted in terms of the small value of the formation constant of the ester intermediate. An another reaction mechanism accounting the acid-catalysis involve the formation of a protonated BIDC prior to formation of an ester intermediate which subsequently decomposes in a slow step leading to the product.

Keywords: benzimidazolium dichromate, benzyl alcohols, correlation analysis, kinetics, oxidation

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Authors: Abd El-Aziz Said

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In this study, natural silica was used as an active, selective, reusable and eco-friendly catalyst for the liquid phase synthesis of iso-amyl, benzyl and cinnamyl esters. The original and calcined natural silica were characterized by TG-DTA, XRF, XRD, FTIR, SEM, and N2-sorption analysis. The surface acidity of the catalysts was determined using isopropanol dehydration and the strength of available acid sites was measured using chemisorption of pyridine (PY) and dimethyl pyridine (DMPY). The results of acidity specified that the acidic sites are of Brönsted type, while PY-TPD demonstrated that almost of the acidic sites over the surface of natural silica are of weak and intermediate strength. The catalytic activity of natural silica towards esterification of acetic acid with alcohols was extensively studied. The results revealed that natural silica had high catalytic activity with 100% selectivity to all targeted esters. In addition, the yields obtained in batch methods were 83, 81, and 80%, respectively, whereas these yields after simple distillation were improved 97, 99.5, and 90%, respectively.

Keywords: liquid-phase esterification, natural silica, acidity esters, characterization

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Authors: Huayang Yu, Nicola Ingram, David C. Green, Paul D. Thornton

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The dual stimuli-controlled release of doxorubicin from gel-embedded nanoparticles is reported. Non-cytotoxic polymer nanoparticles are formed from poly(ethylene glycol)-b-poly(benzyl glutamate) that, uniquely, contain a central ester link. This connection renders the nanoparticles pH-responsive, enabling extensive doxorubicin release in acidic solutions (pH 6.5), but not in solutions of physiological pH (pH 7.4). Doxorubicin loaded nanoparticles were found to be stable for at least 31 days and lethal against the three breast cancer cell lines tested. Furthermore, doxorubicin-loaded nanoparticles could be incorporated within a thermoresponsive poly(2-hydroxypropyl methacrylate) gel depot, which forms immediately upon injection of poly(2-hydroxypropyl methacrylate) into aqueous solution. The combination of the poly(2-hydroxypropyl methacrylate) gel and poly(ethylene glycol)-b-poly(benzyl glutamate) nanoparticles yields an injectable doxorubicin delivery system that facilities near-complete drug release when maintained at elevated temperatures (37 °C) in acidic solution (pH 6.5). In contrast, negligible payload release occurs when the material is stored at room temperature in a non-acidic solution (pH 7.4). The system has great potential as a vehicle for the prolonged, site-specific release of chemotherapeutics.

Keywords: biodegradable, nanoparticle, polymer, thermoresponsive

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Authors: Grazia Disciglio, Francesco Lops, Annalisa Tarantino, Emanuele Tarantino

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The parasitic weed specie Phelipanche ramosa (L) Pomel is one of the major constraints in tomato crop in Apulia region (southern Italy). The experimental was considered to investigate the effect of six organic compounds (Olive miller wastewater, Allil isothiocyanate®, Alfa plus K®, Radicon®, Rizosum Max®, Kendal Nem®) on the naturally infested field of tomato growing season in 2016. The randomized block design with 3 replicates was adopted. Tomato seedling were transplant on 19 May 2016. During the growing cycle of the tomato at 74, 81, 93 and 103 days after transplantation (DAT), the number of parasitic shoots (branched plants) that had emerged in each plot was determined. At harvesting on 13 September 2016 the major quanti-qualitative yield parameters were determined, including marketable yield, mean weight, dry matter, soluble solids, fruit colour, pH and titratable acidity. The treatments provided the results show that none of treatments provided complete control against P. ramosa. However, among the products tested Olive miller wastewater, Alfa plus K®, Rizosum Max® and Kendal Nem® products applied to the soil show the number of emerged shoots significantly lower than Radicon® and especially than the Allil isothiocyanate® treatment and the untreated control. Regarding the effect of different treatments on the tomato productive parameters, the marketable yield resulted significantly higher in the same mentioned treatments which gave the lower P. ramosa infestation. No significative differences for the other fruit characteristics were observed.

Keywords: processing tomato crop, Phelipanche ramosa, olive-mill wastewater, organic fertilizers

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Authors: Hossein Anaraki-Ardakani

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A green and efficient one-pot synthesis of benzylamino coumarin derivatives by a three-component condensation of 4-hydroxycoumarin, cyclic secondary amine, and aromatic aldehyde in the presence of ZrO2 nanoparticles (NPs) as a heterogeneous catalyst in water at room temperature has been reported.

Keywords: 3-benzyl substituted coumarin derivative, ZrO2 nanoparticles (NPs), green synthesis, multicomponent reaction

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Authors: Abobkar Abrahem Mohamed Saad, Asma Abud Alsalam

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Closed flowers of Maerua crassifolia were cultured on Murashige and Skoog medium supplemented with benzyl amino purine BA (1.0 mg/l). The colour of flowers changed from green to pale brown after one week. They opened after two weeks. The anthers became clear which was observed after 3 weeks. Calluses are induced from sepals after one month. 19 anthers were observed with average length of 1.9 cm. The amount of calluses increased after 40 days. These calluses were fragmented and subcultured on MS+ 2-4D (1.0 mg/l) in order to increase growth.

Keywords: in vitro, Maerua, flowers, culture

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Authors: Adel S. El-Azab, Alaa A. M. Abdel-Aziz, Ibrahim A. Al-Suwaidan, Amer M. Alanazi

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A novel series of 2,3,6-trisubstitute quinazolinone were designed, synthesized, and evaluated for their in-vitro antitumor activity. 3 (Benzylideneamino)-6-chloro-2-p-tolylquinazolin-4(3H)-One, 2-[(4-oxo-3-phenethyl-3,4-dihydroquinazolin-2-yl)thio]-N-(3,4;5-trimethoxyphenyl) acetamide and 3-(3-benzyl-6-methyl-4-oxo-3, 4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl) propanamide have shown amazing broad spectrum antitumor activity with mean GI50; 15.8, 3.16, and 7.4 μM respectively compared to known Quinazoline Derivatives antitumor drug 5-FU mean GI50=22.6 μM.

Keywords: quinazoline derivatives, in vitro antitumor, synthesis, 5-FU, NCI

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Authors: J. C. Colmenares, M. Paszkiewicz-Gawron, D. Lomot, S. R. Pradhan, A. Qayyum

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This work is a report of recent selected experiments of photocatalysis intensification using flow microphotoreactors (fabricated by an ultrasound-based technique) for photocatalytic selective oxidation of benzyl alcohol (BnOH) to benzaldehyde (PhCHO) (in the frame of the concept of lignin valorization), and the proof of concept of intensifying a flow selective photocatalytic oxidation process by acoustic cavitation. The synthesized photocatalysts were characterized by using different techniques such as UV-Vis diffuse reflectance spectroscopy, X-ray diffraction, nitrogen sorption, thermal gravimetric analysis, and transmission electron microscopy. More specifically, the work will be on: a Design and development of metal-containing TiO₂ coated microflow reactor for photocatalytic partial oxidation of benzyl alcohol: The current work introduces an efficient ultrasound-based metal (Fe, Cu, Co)-containing TiO₂ deposition on the inner walls of a perfluoroalkoxy alkanes (PFA) microtube under mild conditions. The experiments were carried out using commercial TiO₂ and sol-gel synthesized TiO₂. The rough surface formed during sonication is the site for the deposition of these nanoparticles in the inner walls of the microtube. The photocatalytic activities of these semiconductor coated fluoropolymer based microreactors were evaluated for the selective oxidation of BnOH to PhCHO in the liquid flow phase. The analysis of the results showed that various features/parameters are crucial, and by tuning them, it is feasible to improve the conversion of benzyl alcohol and benzaldehyde selectivity. Among all the metal-containing TiO₂ samples, the 0.5 at% Fe/TiO₂ (both, iron and titanium, as cheap, safe, and abundant metals) photocatalyst exhibited the highest BnOH conversion under visible light (515 nm) in a microflow system. This could be explained by the higher crystallite size, high porosity, and flake-like morphology. b. Designing/fabricating photocatalysts by a sonochemical approach and testing them in the appropriate flow sonophotoreactor towards sustainable selective oxidation of key organic model compounds of lignin: Ultrasonication (US)-assitedprecipitaion and US-assitedhydrosolvothermal methods were used for the synthesis of metal-oxide-based and metal-free-carbon-based photocatalysts, respectively. Additionally, we report selected experiments of intensification of a flow photocatalytic selective oxidation through the use of ultrasonic waves. The effort of our research is focused on the utilization of flow sonophotocatalysis for the selective transformation of lignin-based model molecules by nanostructured metal oxides (e.g., TiO₂), and metal-free carbocatalysts. A plethora of parameters that affects the acoustic cavitation phenomena, and as a result the potential of sonication were investigated (e.g. ultrasound frequency and power). Various important photocatalytic parameters such as the wavelength and intensity of the irradiated light, photocatalyst loading, type of solvent, mixture of solvents, and solution pH were also optimized.

Keywords: heterogeneous photo-catalysis, metal-free carbonaceous materials, selective redox flow sonophotocatalysis, titanium dioxide

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Authors: Dorith Tavor, Adi Wolfson

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In the past two decades a variety of green solvents have been proposed, including water, ionic liquids, fluorous solvents, and supercritical fluids. However, their implementation in industrial processes is still limited due to their tedious and non-sustainable synthesis, lack of experimental data and familiarity, as well as operational restrictions and high cost. Several years ago we presented, for the first time, the use of glycerol-based solvents as alternative sustainable reaction mediums in both catalytic and non-catalytic organic synthesis. Glycerol is the main by-product from the conversion of oils and fats in oleochemical production. Moreover, in the past decade, its price has substantially decreased due to an increase in supply from the production and use of fatty acid derivatives in the food, cosmetics, and drugs industries and in biofuel synthesis, i.e., biodiesel. The renewable origin, beneficial physicochemical properties and reusability of glycerol-based solvents, enabled improved product yield and selectivity as well as easy product separation and catalyst recycling. Furthermore, their high boiling point and polarity make them perfect candidates for non-conventional heating and mixing techniques such as ultrasound- and microwave-assisted reactions. Finally, in some reactions, such as catalytic transfer-hydrogenation or transesterification, they can also be used simultaneously as both solvent and reactant. In our ongoing efforts to design a viable protocol that will facilitate the acceptance of glycerol and its derivatives as sustainable solvents, pure glycerol and glycerol triacetate (triacetin) as well as various glycerol-triacetin mixtures were tested as sustainable solvents in several representative organic reactions, such as nucleophilic substitution of benzyl chloride to benzyl acetate, Suzuki-Miyaura cross-coupling of iodobenzene and phenylboronic acid, baker’s yeast reduction of ketones, and transfer hydrogenation of olefins. It was found that reaction performance was affected by the glycerol to triacetin ratio, as the solubility of the substrates in the solvent determined product yield. Thereby, employing optimal glycerol to triacetin ratio resulted in maximum product yield. In addition, using glycerol-based solvents enabled easy and successful separation of the products and recycling of the catalysts.

Keywords: glycerol, green chemistry, sustainability, catalysis

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Authors: Vivek Singh Bhadauria, Abhishek Pandey

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Indole-2,3-diones are known for their various biological activities. By suitable control of a substituent, different novel indole-2,3-diones were synthesized. In this present study, various Schiff and Mannich bases were synthesized and characterized, and evaluated their for different pharmacological activities. The compounds were prepared by reacting indole-2,3-dione with benzyl chloride and 4-substituted thiosemicarbazides. All the synthesized compounds were characterized by the TLC, MP, Elemental analysis, FTIR, 1H-NMR and Mass spectroscopy. The compounds have been evaluated for their anticancer, antituberculosis, anticonvulsant, antiinflammatory as well as anti-SARS activity and the results are presented. Some of compounds possessed different pharmacological activity at a concentration of 200 mg/kg body weight and even at lower concentration.

Keywords: indoles, isatin, NMR, biological activities

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Authors: Krishna Poudel, Tahar Katuwal, Sujan Karki

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A rapid propagation and acclimatization method of large cardamom was optimized in this study. Sprouted rhizome buds were collected. The excised rhizome bud explants were cultured on semi solid culture media. The explants were cultured on Murashige and Skoog’s (MS) medium supplemented with different concentration and combinations of BAP (6-Benzyl-amino-purine) and IBA (Indole-3-butyric acid) for shoot and root induction. Explants cultured on MS basal medium supplemented with 1.0 mg/l BAP + 0.5 gm/l IBA showed the highest rate of shoot multiplication. In vitro shoots were rooted on to the half-strength MS basal media supplemented with 0.5 mg/l IBA. Rooted shoots were transplanted in the screen house for hardening process. These hardened plants were subsequently shifted into the netted nursery for further multiplication process.

Keywords: concentration, explants, hardening, rhizome

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Authors: Nasser R. El-Brollosy, Roberta Loddo

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6-Benzyl-1-(ethoxymethyl)-5-isopropyluracil (Emivirine) and its corresponding 1-benzyloxymethyl analogue (TNK-651) showed high activity against HIV-1. The present study describes synthesis of novel emivirine analogues by reaction of chloromethyl ethyl ether with uracils having 5-ethyl / isopropyl and 6-(3,5-dimethoxybenzyl) substituents. A series of new TNK-651 analogues substituted at N-1 with phenoxyethoxymethyl moiety was prepared on treatment of the corresponding uracils with bis(phenoxyethoxy) methane. The newly synthesized non-nucleosides were tested for biological activity against wild type HIV-1 IIIB as well as the resistant strains N119 (Y181C), A17 (K103N + Y181C), and the triple mutant EFVR (K103R + V179D + P225H) in MT-4 cells. Some of the tested compounds showed good activities. Among them 6-(3,5-dimethylbenzyl)-5-ethyl-1-[2-(phenoxyethyl) oxymethyl]uracil which showed inhibitory potency higher than emivirine against both wild type HIV-1 and the tested mutant strains.

Keywords: Emivirine, HIV, non-nucleoside reverse transcriptase, uracils

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Authors: Mitakshara Sharma, Sonal Sharma

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Vesiculobullous diseases are heterogeneous group of dermatological disorders with protean manifestations. The most important technique for the patients with vesiculobullous diseases is conventional histopathology and confirmatory tests like direct immunofluorescence (DIF) and indirect immunofluorescence (IIF). DIF has been used for decades to investigate pathophysiology and in the diagnosis. It detects molecules such as immunoglobulins and complement components. It is done on the perilesional skin. Diagnosis of DIF test depends on features like primary site of the immune deposits, class of immunoglobulin, number of immune deposits and deposition at other sites. The aim of the study is to correlate DIF with clinical and histopathological findings and to analyze the utility of DIF in the diagnosis of these disorders. It is a retrospective descriptive study conducted for 2 years from 2015 to 2017 in Department of Pathology, GTB Hospital on perilesional punch biopsies of vesiculobullous lesions. Biopsies were sent in Michael’s medium. The specimens were washed, frozen and incubated with fluorescein isothiocyanate (FITC) tagged antihuman antibodies IgA, IgG, IgM, C3 & F and were viewed under fluorescent microscope. Out of 401 skin biopsies submitted for DIF, 285 were vesiculobullous diseases, in which the most common was Pemphigus vulgaris (34%) followed by Bullous pemphigoid (21.5%), Dermatitis herpetiformis (16%), Pemphigus foliaceus (11.9%), Linear IgA disease (11.9%), Epidermolysisbullosa (2.39%) and Pemphigus herpetiformis (1.7%). We will be presenting the DIF findings in the all these vesiculobullous diseases. DIF in conjugation with histopathology gives the best diagnostic yield in these lesions. It also helps in the diagnosis whenever there is a clinical and histopathological overlap.

Keywords: antibodies, direct immunofluorescence, pemphigus, vesiculobullous

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Authors: Uchechukwu Vincent Okpala

Abstract:

Under the Sun, energy is a key factor for the sustenance of life and its environment. The need to protect the environment as energy is generated and consumed has called for renewable and green energy sources. To be part of this green revolution, we synthesized and characterized undoped and velvet tamarind doped zinc sulfide (ZnS) crystals using sol-gel methods. Velvet tamarind was whittled down using the top-down approach of nanotechnology. Sodium silicate, tartaric acid, zinc nitrate, and thiourea were used as precursors. The grown samples were annealed at 105°C. Structural, optical, and compositional analyses of the grown samples revealed crystalline structures with varied crystallite sizes influenced by doping. Energy-dispersive X-ray spectroscopy confirmed elemental compositions of Zn, S, C and O in the films. Atomic percentages of the elements varied with VT doping. FT-IR analysis indicated the presence of functional groups like O-H stretching (alcohol), C=C=C stretching (alkene group), C=C bending, C-H stretching (alkane), N-H stretching (aliphatic primary amine) and N=C=S stretching (isothiocyanate) constituent in the film. The transmittance of the samples increased from the visible region to the infrared region making the samples good for poultry and solar energy applications. The bandgap energy of the films decreased as the number of VT drops increased, from 2.4 to 2.2. They were wide band gap materials and were good for optoelectronic, photo-thermal, high temperature, high power and solar cell applications.

Keywords: doping, sol-gel, velvet tamarind, ZnS.

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Authors: Gurpreet Kaur, Manoj Kumar, Vandana Bhalla

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Strong acceptor-weak acceptor system FN-TPy has been designed and synthesized which undergoes solvent dependent self-assembly in mixed aqueous media to generate through space intermolecular charge transfer assemblies. The as prepared entropically favoured assemblies of FN-TPy exhibit excellent photostability and photosensitizing properties in the assembled state to activate aerial oxygen for efficient generation of reactive oxygen species (ROS) through Type-I and Type-II pathways. The FN-TPy assemblies exhibit excellent potential for regulated oxidation of alcohols and aldehydes under mild reaction conditions (visible light irradiation, aqueous media, room temperature) using aerial oxygen as the ‘oxidant’. The present study demonstrates the potential of FN-TPy assemblies to catalyze controlled oxidation of benzyl alcohol to benzaldehyde and to corresponding benzoic acid.

Keywords: oxidations, photosensitizer, reactive oxygen species, supramolecular assemblies, through space charge transfer.

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Authors: Atul Kumar, Veeranjaneyulu Gannedi, Qazi Naveed Ahmed

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Oligosaccharides, which are essential to all cellular organisms, play vital roles in cell recognition, signaling, and are involved in a broad range of biological processes. The chemical synthesis of carbohydrates represents a powerful tool to provide homogeneous glycans. In carbohydrate synthesis, the major concern is the orthogonal protection of hydroxyl groups that can be unmasked independently. Classical protecting groups include benzyl ethers (Bn), which are normally cleaved through hydrogenolysis or by means of metal reduction, and acetate (Ac), benzoate (Bz) or pivaloate esters, which are removed using base promoted hydrolysis. In present work a series of α-Oxoester (COBz) protected saccharides, with divergent base sensitivity profiles against benzoyl (Bz) and acetyl (Ac), were designed and KHSO₅/CH₃COCl in methanol was identified as an easy, mild, selective and efficient deprotecting reagent for their removal in the perspective of carbohydrate synthesis. Timely monitoring of later reagent was advantageous in establishing both sequential as well as simultaneous deprotecting of COBz, Bz, and Ac. The salient feature of our work is its ease to generate different acceptors using designed monosaccharides. In summary, we demonstrated α-Oxoester (COBz) as a new protecting group for carbohydrates and the application of this group for the synthesis of Glycosylphosphatidylinositol (GPI) anchor are in progress.

Keywords: α-Oxoester, oligosaccharides, new protecting group, acceptor synthesis, glycosylation

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Authors: Kristine Vike-Jonas, Susana V. Gonzalez, Olav L. Bakkerud, Karoline S. Gjelstad, Shazia N. Aslam, Øyvind Mikkelsen, Alexandros Asimakopoulos

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P-hydrobenzoic acid esters (parabens), paraben metabolites, and triclocarban (TCC) are a group of synthetic antimicrobials classified as endocrine disrupting chemicals (EDCs) and emerging pollutants. The aim of this study was to investigate the levels of these compounds in sediment near the effluent of a wastewater treatment plant (WWTP) in the Trondheim Fjord, Norway. Paraben, paraben metabolites, and TCC are high volume production chemicals that are found in a range of consumer products, especially pharmaceuticals and personal care products (PCPs). In this study, six parabens (methyl paraben; MeP, ethyl paraben; EtP, propyl paraben; PrP, butyl paraben; BuP, benzyl paraben; BezP, heptyl paraben; HeP), four paraben metabolites (4-hydroxybenzoic acid; 4-HB, 3,4-dihydroxybenzoic acid; 3,4-DHB, methyl protocatechuic acid; OH-MeP, ethyl protocatechuic acid; OH-EtP) and TCC were determined by ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) in 64 sediment samples from 10 different locations outside Trondheim, Norway. Of these 11 target analytes, four were detected in 40 % or more of the samples. The sum of six parabens (∑Parabens), four paraben metabolites (∑Metabolites) and TCC in sediment ranged from 4.88 to 11.56 (mean 6.81) ng/g, 52.16 to 368.28 (mean 93.89) ng/g and 0.53 to 3.65 (mean 1.50) ng/g dry sediment, respectively. Pearson correlation coefficients indicated that TCC was positively correlated with OH-MeP, but negatively correlated with 4-HB. To the best of the author’s knowledge, this is the first time parabens, paraben metabolites and TCC have been reported in the Trondheim Fjord.

Keywords: parabens, liquid chromatography, sediment, tandem mass spectrometry

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Authors: Ipek Gunay, Efe B. Orman, Metin Ozer, Bekir Salih, Ali R. Ozkaya

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Phthalocyanines with macrocyclic ring containing at least three heteroatoms have nine or more membered structures. Metal-free phthalocyanines react with metal salts to obtain chelate complexes. This is one of the most important features of metal-free phthalocyanine as ligand structure. Although phthalocyanines have very similar properties with porphyrins, they have some advantages such as lower cost, easy to prepare, and chemical and thermal stability. It’s known that Pc compounds have shown one-electron metal-and/or ligand-based reversible or quasi-reversible reduction and oxidation processes. The redox properties of phthalocyanines are critically related to the desirable properties of these compounds in their technological applications. Thus, Pc complexes have also been receiving increasing interest in the area of fuel cells due to their high electrocatalytic activity in dioxygen reduction and fuel cell applications. In this study, novel phthalocyanine complexes coordinated with Fe(II) and Co (II) to be used as catalyst were synthesized. Aiming this goal, a new nitrile ligand was synthesized starting from 4-hydroxy-3,5-dimethoxy benzyl alcohol and 4-nitrophthalonitrile in the presence of K2CO3 as catalyst. After the isolation of the new type of nitrile and metal complexes, the characterization of mentioned compounds was achieved by IR, H-NMR and UV-vis methods. In addition, the electrochemical behaviour of Pc complexes was identified by cyclic voltammetry, square wave voltammetry and in situ spectroelectrochemical measurements. Furthermore, the catalytic performances of Pc complexes for oxygen reduction were tested by dynamic voltammetry measurements, carried out by the combined system of rotating ring-disk electrode and potentiostat, in a medium similar to fuel-cell working conditions.

Keywords: phthalocyanine, electrocatalysis, electrochemistry, in-situ spectroelectrochemistry

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Authors: Abobakr Khidir Ziyada, Cecilia Devi Wilfred

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In the present work, a new series of 3-propanenitrile imidazolium-based Room Temperature Ionic Liquids (RTILs), incorporating dioctyl sulfosuccinate (DOSS) were prepared by reacting imidazole with acrylonitrile and then reacting the product with allyl chloride, 2-chloroethanol, and benzyl chloride. After the reaction had been completed, metathesis reaction was carried out using sodium dioctyl sulfosuccinate. The densities and viscosities of the present RTILs were measured at atmospheric pressure at T=293.15 to 353.15 K, the refractive index was measured at T=293.15 to 333.15 K, whereas, the start and decomposition temperatures were determined at heating rate 10°C. min^-1. The thermal expansion coefficient, densities at a range of temperatures and pressures, molecular volume, molar refraction, standard entropy and the lattice energy of these RTILs were also estimated. The present RTILs showed higher densities, similar refractive indices, and higher viscosities compared to the other 1-alkyl-3-propanenitrile imidazolium-based RTILs. The densities of the present synthesized RTILs are lower compared to the other nitrile-functionalized ILs. These present RTILs showed a weak temperature dependence on the thermal expansion coefficients, αp=5.0 × 10^−4 to 7.50 × 10−4 K^-1. Empirical correlations were proposed to represent the present data on the physical properties. The lattice energy for the present RTILs was similar to other nitrile–based imidazolium RTILs. The present RTILs showed very high molar refraction when compared similar RTILs incorporating other anions.

Keywords: dioctyl sulfosuccinate, nitrile ILs, 3-propanenitrile, anion, room temperature ionic liquids, RTIL

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Authors: Ozlem Bahadir Acikara, Mert Ilhan, Ekin Kurtul, Karel Smejkal, Esra Kupeli Akkol

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Present study is aimed to investigate in vitro inhibitory effects of the extracts prepared from the aerial parts of Podospermum canum (Asteraceae) on hyaluronidase, collagenase, and elastase enzymes using a bioassay-guided fractionation. Inhibitory effects of the extract, sub-extracts, fractions obtained by column chromatography, and isolated compounds on collagenase, elastase, and hyaluronidase were performed by using in vitro enzyme inhibitory assays based on spectrophotometric evaluation. The ethyl acetate and remaining water extracts prepared from the plant displayed significant inhibitory activities on collagenase and elastase, while petroleum ether and chloroform extracts did not show any inhibitory activity. Eleven known compounds: arbutin, 6'-O-caffeoylarbutin, cichoriin, 3,5-dicaffeoylquinic acid methyl ester, apigenin-7-O-β-glucoside, luteolin-7-O-β-glucoside, apigenin-7-O-β-rutinoside, isoorientin, orientin, vitexin, procatechuic acid, and compound 4-hydroxy-benzoic acid 4-(6-O-α-rhamnopyranosyl-β-glucopyranosyl) benzyl ester have been obtained from ethyl acetate sub-extract of the plant through bioassay-guided fractionation and isolation. Results of the present study have revealed that among the isolated compounds, apigenin-7-O-β-glucoside, luteolin-7-O-β-glucoside, apigenin-7-O-β-rutinoside and isoorientin showed potent enzyme inhibitory activities. However, methanolic extract of P. canum displayed a greater inhibitory activity than fractions and isolated compounds both on collagenase and elastase.

Keywords: Asteraceae, collagenase, elastase, hyaluronidase, Podospermum canum

Procedia PDF Downloads 93