Senthilkumar, Palaniappan ; Dinakaran, Murugesan ; Yogeeswari, Perumal ; China, Arnab ; Nagaraja, V. ; Sriram, Dharmarajan (2009) Antimycobacterial activities of novel fluoroquinolones Biomedicine & Pharmacotherapy, 63 (1). pp. 27-35. ISSN 0753-3322
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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S07533...
Related URL: http://dx.doi.org/10.1016/j.biopha.2007.10.004
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 (MC2) 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 (7l) was found to be the most active compound in vitro with MIC of 0.09 μM against MTB and MDR-TB respectively. In the in vivo animal model 7l 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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Antitubercular Activity; Antimycobacterial Activity; Quinolones; Fluoroquinolones; DNA Gyrase Inhibitors |
| ID Code: | 27009 |
| Deposited On: | 08 Dec 2010 12:51 |
| Last Modified: | 08 Jun 2011 06:56 |
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