4.7 Article

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 16, Pages 6063-6072

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.06.051

Keywords

Mycobacterium tuberculosis; Hydrazone; Quinoline

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A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 mu g/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results. (C) 2009 Elsevier Ltd. All rights reserved.

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