Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 2
Search results for: Eskedar Lodebo
2 Pyrazolylpyrazolines: Design, Synthesis and Biological Evaluation as Dual Acting Antimalarial-Antileishmanial Agents
Authors: Adnan Bekhit, Eskedar Lodebo, Ariaya Hymete, Hanan Ragab, Alaa El-Din Bekhit
Abstract:
Malaria and leishmaniasis have emerged as serious universal health problems throughout history of mankind. According to the WHO 2008 malarial report, half of the world population is at risk of malarial infection with an estimate of 1 million deaths occurring annually mainly in the African region. Furthermore, 12-15 million people are infected with Leishmaniasis worldwide. Despite the continuous introduction of a large number of agents for the treatment of malaria, there is still unmet medical needs due to the emergence of resistance. Resistance has occurred for almost all therapeutic agents approved for the treatment of malaria. Accordingly, it was the aim of this work to design and synthesis a group of antimalarial-antileshmanial agents that would show inhibitory activity against chloroquine-resistant strain of Plasmodium falciparum. The synthesized compounds were designed to contain a pyrazolylpyrazoline moiety having an aromatic group (p-tolyl or p-chlorophenyl) at N1-position of one pyrazoline ring due to the reports of promising activities of such compounds. A formyl or acyl substituent was introduced at the N1-position of the other pyrazoline ring, to investigate the effect of bulkiness of acyl substituents at this position. The synthesized compounds were evaluated for their in-vivo antimalarial activity against Plasmodium berghei infected mice at dose levels of 20 and 30 mg/Kg. the two most active compounds were evaluated for their antimalarial activity against chloroquin-resistant strain (RKL9) of Plasmodium falciparum. In addition, the synthesized compounds were tested for their in-vitro antileshmanial activity against Leishmania aethiopica promastigotes and amastigotes. For both antimalarial and antileishmanial activities, compounds having an N1-p-tolyl group at the first pyrazoline ring did not require bulkiness at the second pyrazoline ring nitrogen where the compound bearing an acetyl group proved to be the most active of the whole series. On the other hand, bulkiness at the N1-position of the second pyazoline ring was necessary in case of compounds carrying the p-chlorophenyl group, where the two derivatives having an N1-butanoyl and an N1-benzoyl moieties at the second pyrazoline showed the best activity. Furthermore, the toxicity of the active compounds were tested and were proved to be non-toxic at 125, 250 and 500 mg/Kg. In addition, docking of the most active compound (having a p-tolyl group at the first pyrazoline-N and an acetyl moiety on the other pyrazoline-N) was performed against dihydrofolate reductase enzyme.Keywords: pyrazoline derivatives, in-vivo antimalarial activity, docking, dihydrofolate reductase
Procedia PDF Downloads 3411 A Study on the Problems of Sports Commitment and Athlete Satisfaction of Oromia League Football Clubs in Case of West, East and Horro Guduru Wollega Zones, Ethiopia
Authors: Biruk Hundito Lodebo
Abstract:
The main purpose of this study was to investigate the problems of sports commitment and athlete satisfaction of Oromia league football clubs in the West, East and Horro Guduru wollega zones. The descriptive survey method was designed and approached as a quantitative method. The data was collected by questionnaires. The research data was collected from sports commitment and athlete satisfaction variables. The target population of this study was (3x30=90) and the researcher selected by using purposive sampling techniques. The data were analysed by SPSS Software (Version 20). Such as mean standard deviation, one-way ANOVA and correlational analysis. The level of significance is 0.05 alpha level. The researchers' hypothesis of this study was: (1) There is no significant difference between sports commitments and player satisfaction indices in all selected Oromia league football wollega zones. (2)There is no significant difference between sports commitments and player satisfaction indices in all selected Oromia league football wollega zones.(3)There is no correlation between the variables of sports commitments and player satisfaction indices in all selected Oromia league football wollega zones. Finally, the study findings indicated that: (a) There is no significant difference between sports commitment and athlete satisfaction of Oromia league football clubs. (b) There is no significant difference between player age and sports commitment in Oromia league football clubs in the West, East and Horro Guduru wollega zones. (c) There is no significant difference between player age and athlete satisfaction in Oromia league football clubs in the West, East and Horro Guduru wollege zones. Based on the research findings the following recommendations were forwarded: The club management and players should be made a positive linkage and improvement between sports commitments and player satisfaction, All clubs management staff and coaching staff should promote Sports commitment and player satisfaction. Workshops and short-term training can be held for all of sports management staff and players.Keywords: sports commetmnet, Athet satisfaction, football, Oromia league
Procedia PDF Downloads 103