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Substituted 4-methylquinolines as a new class of anti-tuberculosis agents

We report synthesis and anti-tuberculosis activities of a series of novel ring-substituted quinolines. The most effective compound of the series 3d (MIC=6.25 μg/mL, Mycobacterium tuberculosis H37Rv strain) was synthesized in one step; thus is an attractive lead molecule for anti-tuberculosis drug de...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-03, Vol.13 (6), p.1051-1054
Main Authors: Jain, Rahul, Vaitilingam, Balasubramanian, Nayyar, Amit, Palde, Prakash B
Format: Article
Language:English
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Summary:We report synthesis and anti-tuberculosis activities of a series of novel ring-substituted quinolines. The most effective compound of the series 3d (MIC=6.25 μg/mL, Mycobacterium tuberculosis H37Rv strain) was synthesized in one step; thus is an attractive lead molecule for anti-tuberculosis drug development. The results of this study represent the discovery of ring-substituted 4-methylquinolines as new class of potential anti-tuberculosis agents. The synthesis and antimycobacterial activities ( Mycobacterium tuberculosis H37Rv strain) for a series of ring-substituted 4-methylquinolines are described. The evaluation of cytotoxicity and efficacy against M. avium and single-drug-resistant (SDR) strains of M. tuberculosis for the most effective compound 3d ( R= c-C 5H 9) are also reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00074-X