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Synthesis and antimycobacterial evaluation of various 7-substituted ciprofloxacin derivatives

Sriram, Dharmarajan and Yogeeswari, Perumal and Basha, Jafar Sadik and Radha, Deshpande R and Nagaraja, Valakunja (2005) Synthesis and antimycobacterial evaluation of various 7-substituted ciprofloxacin derivatives. In: Bioorganic & Medicinal Chemistry, 13 (20). pp. 5774-5778.

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Tuberculosis continues to be a major cause of morbidity and mortality all over the world. Various 7-substituted ciprofloxacin derivatives were synthesized and evaluated for antimycobacterial activity in vitro and in vivo against Mycobacterium tuberculosis and for inhibition ofthe supercoiling activity of DNA gyrase from Mycobacterium smegmatis.Preliminary results indicated that most of the compounds demonstrated better in vitro antimycobacterial activity against M. tuberculosis than ciprofloxacin. Compound1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-[[N-4-[1'-(5-methylisatinyl-ss-semicarbazo)]methyl]N'-piperazinyl]-3-quinolinecarboxylic acid (3h) decreased the bacterial load in spleen tissue with 0.76-log(10) protections and was considered to be moderately active in reducing bacterial count in spleen. The results demonstrated the potential and importance of developing new quinolone derivatives against mycobacterial infections.

Item Type: Journal Article
Publication: Bioorganic & Medicinal Chemistry
Publisher: Pergamon-Elsevier Science Ltd
Additional Information: Copyright for this article belongs to Elsevier.
Keywords: Antimycobacterial;Anti-TB;Ciprofloxacin derivatives;DNA gyrase inhibition
Department/Centre: Division of Biological Sciences > Microbiology & Cell Biology
Date Deposited: 11 Nov 2005
Last Modified: 19 Sep 2010 04:21
URI: http://eprints.iisc.ac.in/id/eprint/3992

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