Bioorganic & Medicinal Chemistry Letters 2012-01-01

Novel 2-(2-(4-aryloxybenzylidene) hydrazinyl)benzothiazole derivatives as anti-tubercular agents.

Vikas N Telvekar, Vinod Kumar Bairwa, Kalpana Satardekar, Anirudh Bellubi

文献索引：Bioorg. Med. Chem. Lett. 22 , 649-52, (2012)

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摘要

A series of structurally novel, substituted 2-(2-(4-aryloxybenzylidene) hydrazinyl)benzothiazole derivatives incorporating 2-hydrazinyl benzothiazole and 4-(aryloxy)benzaldehyde were designed and synthesized using molecular hybridization approach. All the synthesized compounds exhibited promising activity (MIC 1.5-29.00μg/ml) against Mycobacteriumtuberculosis H37Rv strains of using REMA. Five of the evaluated compounds exhibit MIC <3.0μg/ml. Compound (E)-6-chloro-2-(2-(4-(2,4-dichlorophenoxy)benzylidene)hydrazinyl) benzothiazole showed MIC of 1.5μg/ml. Thus, this compound could act as a potential lead for further development of new anti-tubercular drugs.Copyright © 2011 Elsevier Ltd. All rights reserved.