Antimycobacterial activities of novel fluoroquinolones

Senthilkumar, Palaniappan and Dinakaran, Murugesan and Yogeeswari, Perumal and china, Arnab and Nagaraja, Valakunja and Sriram, Dharmarajan (2009) Antimycobacterial activities of novel fluoroquinolones. In: Biomedicine & Pharmacotherapy, 63 (1). pp. 27-35.

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Abstract

Fifty-one novel 1-(cyclopropyl/2,4-difluorophenyl/t-butyl)-1,4-dihydro-6-fluoro-7-(sub secondary amino)-4-oxoquinoline-3-carboxylic acids were synthesized and evaluated for their antimycobacterial in vitro and in vivo against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant Mycobacterium tuberculosis (MDR-TB) and Mycobacterium smegmatis (MC 2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from M. smegmatis. Among the synthesized compounds, 7-(3-(diethylcarbamoyl)piperidin-1-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (7I) was found to be the most active compound in vitro with MIC of 0.09 mu M against MTB and MDR-TB respectively. In the in vivo animal model 7I decreased the mycobacterial load in lung and spleen tissues with 2.53- and 4.88-log10 protections respectively at a dose of 50 mg/kg body weight. (C) 2007 Elsevier Masson SAS. All rights reserved.

Item Type:	Journal Article
Publication:	Biomedicine & Pharmacotherapy
Publisher:	Elsevier Science
Additional Information:	Copyright belongs of this article belongs to Elsevier Science.
Keywords:	Antitubercular activity; Antimycobacterial activity; Quinolones; Fluoroquinolones; DNA gyrase inhibitors
Department/Centre:	Division of Biological Sciences > Microbiology & Cell Biology
Date Deposited:	27 May 2009 10:20
Last Modified:	19 Sep 2010 05:31
URI:	http://eprints.iisc.ac.in/id/eprint/20013

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