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标题：Design and synthesis of 3-(4-aminophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1 H-pyrazole-1-carboxamide/carbothioamide analogues as antitubercular agents
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作者：Mohamed Jawed Ahsan ; Mohamed Jawed Ahsan ; Veerendra Saini 等
期刊名称：Beni-Suef University Journal of Basic and Applied Sciences
印刷版ISSN：2314-8535
电子版ISSN：2314-8543
出版年度：2015
卷号：4
期号：1
页码：41-46
DOI：10.1016/j.bjbas.2015.02.006
语种：English
出版社：Elsevier
摘要：AbstractEmergence of multi-drug resistant tuberculosis (MDR-TB) and HIV-TB co-infections potentiate the development of newer antitubercular agents to combat against tuberculosis, a dreadful disease. In the present investigation a series of pyrazoline analogues were designed and synthesized based on the structure of known antitubercular agent thiacetazone, in hope of obtaining new and safe antitubercular agents. The target molecules were synthesized in two steps, starting with the condensation of 4-aminoacetophenone andp-anisidine in methanolic sodium hydroxide solution followed by the cyclization of intermediate chalcones with appropriate semicarbazide/thiosemicarbazide in glacial acetic acid. All the synthesized compounds were characterized by1H NMR, IR and mass spectral data and the purity of the compounds was checked by elemental analysis. Their antimycobacterial activity was evaluated by two folds serial dilution method. 3-(4-Aminophenyl)-N-(4-chlorophenyl)-4,5-dihydro-5-(4-methoxyphenyl)pyrazole-1-carboxamide (4i) showed maximum activity againstMycobacterium tuberculosisH37Rv with minimum inhibitory concentration (MIC) of 7.41 μM.
关键词：Antitubercular agents;Claisen Schmidt condensation;Pyrazolines