4.5 Article

Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 22, Pages 6272-6274

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.098

Keywords

Tuberculosis; Quinoline; Drugs

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A series of twenty-one 7-chloro-4-quinolinylhydrazones (3a-u) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv. The compounds 3f, 3i and 3o were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity (2.5 mu g/mL), which can be compared with that of the first line drugs, ethambutol (3.12 mu g/mL) and rifampicin (2.0 mu g/mL). These results can be considered an important start point for the rational design of new leads for anti-TB compounds. (C) 2009 Elsevier Ltd. All rights reserved.

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