Synthesis and antimycobacterial screening of new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives

查看全文 作　　者：Nagabhushana [1]Nayak;Jurupula [1]Ramprasad;Udayakumar [1]Dalimba;Perumal [2]Yogeeswari;Dharmarajan [2]Sriram

机构地区：[1]Organic Chemistry Laboratory,Department of Chemistry,National Institute of Technology Karnataka;[2]Medicinal Chemistry and Drug Discovery Research Laboratory,Pharmacy Group,Birla Institute of Technology and Science-Pilani,Hyderabad Campus

出　　处：《Chinese Chemical Letters》索引2016年第27卷第3期,共5页

基　　金：National Institute of Technology Karnataka,India for the financial support and laboratory facility 摘　　要：This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives(8a–x). The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv(MTB) revealed that 2-chloro-N-(4-(5-(4-chlorophenyl)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)benzamide(8n) is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative(8o) is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity(MIC = 3.13 mg/m L). Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development. 关键词：酰胺衍生物氯苯基吡唑基药物筛选抗微生物合成结核分枝杆菌活性化合物

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Synthesis and antimycobacterial screening of new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives

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