Evaluation of antimycobacterial and DNA gyrase inhibition of fluoroquinolone derivatives

Sriram, Dharmarajan and Bal, Tanushree Ratan and Yogeeswari, Perumal and Radha, Deshpande R and Nagaraja, Valakunja (2006) Evaluation of antimycobacterial and DNA gyrase inhibition of fluoroquinolone derivatives. In: Journal of General and Applied Microbiology, 52 (4). pp. 195-200.

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Abstract

The antimycobacterial activity (both in vitro and in vivo) and DNA gyrase inhibition of newly synthesized fluoroquinolone derivatives were tested against Mycobacterium tuberculosis $H_{37}$Rv and Mycobacterium smegmatis, respectively. Among the synthesized compounds, compound F11 was found to exhibit the most potent in vitro antimycobacterial activity with a MIC value of 0.78 μg/ml, and a selectivity index of more than 80 while not being cytotoxic to the Vero cell line up to 62.5 μg/ml. When evaluated for in vivo antimycobacterial activity, compound F11 demonstrated a paramount decrease of bacterial load in lung and spleen tissues compared to the control and better than the standard drug ciprofloxacin.

Item Type:	Journal Article
Additional Information:	Copyright of this article belongs to Microbiology Research Foundation.
Keywords:	DNA gyrase inhibition;Fluoroquinolone derivatives;Isatin derivatives;Mycobacterium smegmatis;Mycobacterium tuberculosis.
Department/Centre:	Division of Biological Sciences > Microbiology & Cell Biology
Date Deposited:	11 Aug 2008
Last Modified:	19 Sep 2010 04:38
URI:	http://eprints.iisc.ernet.in/id/eprint/11397

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