Synthesis and evaluation of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-(2-(4-substitutedpiperazin-1-yl)acetyl)piperazin-1-yl)quinoline-3-carboxylic acid derivatives as anti-tubercular and antibacterial agents

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• 作者：Narva Suresh ; Hunsur Nagendra Nagesh ; Janupally Renuka ; Vikrant Rajput ; Rashmi Sharma ; Inshad Ali Khan ; Ch ; ra Sekhar Kondapalli Venkata Gowri
• 关键词：Fluoroquinolone ; Anti-tubercular activity ; Antibacterial activity ; Cytotoxicity ; Supercoiling assay
• 刊名：European Journal of Medicinal Chemistry
• 出版年：7 January, 2014
• 年：2014
• 卷：71
• 期：Complete
• 页码：324-332
• 全文大小：588 K

文摘

A series of twenty two novel 1-cyclopropyl-6-fluoro-4-oxo-7-(4-substitutedpiperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid analogues were synthesized, characterized (¹H NMR, ¹³C NMR and LCMS) and screened for their in聽vitro anti-tubercular and antibacterial activity. Many of these compounds exhibited MIC values in the range 7.32-136.10聽渭M against Mycobacterium tuberculosis H₃₇Rv. Eight compounds were further subjected to cytotoxic studies. Furthermore, the title compounds were screened for antibacterial activity against Staphylococcus aureus ATCC 29213 (gram positive) and Escherichia coli ATCC 25922 (gram negative) bacteria. Many of these compounds exhibited MIC values in the range 0.44-34.02聽渭M. Compound 3f was found to be the most active with an MIC of 0.44 and 0.8聽渭M respectively against both the strains. In general, the antibacterial activity of title compounds was more prominent.