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新型2-(2-亚苄基肼基)苯并[d]噻唑作为潜在的抗结核药物。

Novel 2-(2-benzylidenehydrazinyl)benzo[d]thiazole as potential antitubercular agents.

作者信息

Bairwa Vinod Kumar, Telvekar Vikas N

机构信息

Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, India.

出版信息

Comb Chem High Throughput Screen. 2013 Mar;16(3):244-7. doi: 10.2174/1386207311316030009.

Abstract

Molecular hybridization approach was used to synthesize substituted 2-(2-(4-aryl oxy benzylidene) hydrazinyl)benzo thiazole derivatives with 2-hydrazinobenzothiazole and 4-(alicycli/aryl/biaryl/heteroaryl oxy)benzaldehyde as new anti-TB agents. The synthesized compounds, when tested against H37Rv strains of Mtb using Resazurin Microtitre Assay (REMA) method, showed promising activity (MIC 1.35-36.50 μg/mL). 6-chloro-2-(2-(4- (pyridin-4-yloxy) benzylidene) hydrazinyl) benzo[d]thiazole (10v) gave MIC of 1.35 μg/mL. Thus making it, a potential lead could be developed for further antitubercular studies.

摘要

采用分子杂交方法,以2-肼基苯并噻唑和4-(脂环族/芳基/联芳基/杂芳基氧基)苯甲醛为原料合成了取代的2-(2-(4-芳氧基亚苄基)肼基)苯并噻唑衍生物,作为新型抗结核药物。使用刃天青微量滴定法(REMA)对合成的化合物针对结核分枝杆菌H37Rv菌株进行测试时,显示出有前景的活性(MIC为1.35 - 36.50μg/mL)。6-氯-2-(2-(4-(吡啶-4-基氧基)亚苄基)肼基)苯并[d]噻唑(10v)的MIC为1.35μg/mL。因此,它有可能被开发为进一步抗结核研究的潜在先导化合物。

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