4.5 Article

Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 3, Pages 1040-1044

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.045

Keywords

Quinoline-3-carbohydrazone; TMC 207; Antituberculosis activity; (3R)-3-Amino-N,N-dimethyl-4-(phenylthio)butanamide

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A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modi. cations to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis. (C) 2009 Elsevier Ltd. All rights reserved.

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