期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 3, 页码 1040-1044出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.045
关键词
Quinoline-3-carbohydrazone; TMC 207; Antituberculosis activity; (3R)-3-Amino-N,N-dimethyl-4-(phenylthio)butanamide
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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