4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 1, Pages 649-652

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.064

Keywords

Tuberculosis; 2-Hydrazinyl benzothiazole; Molecular hybridization; 4-(Aryloxy)benzaldehyde

Funding

  1. Department of Science & Technology (DST), Government of India, New Delhi

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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 1.5-29.00 mu g/ml) against Mycobacterium tuberculosis H37Rv strains of using REMA. Five of the evaluated compounds exhibit MIC <3.0 mu g/ml. Compound (E)-6-chloro-2-(2-(4-(2,4-dichlorophenoxy) benzylidene) hydrazinyl) benzothiazole showed MIC of 1.5 mu g/ml. Thus, this compound could act as a potential lead for further development of new anti-tubercular drugs. (C) 2011 Elsevier Ltd. All rights reserved.

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