合成与评价 1-环丙基-6-氟-1,4-二氢-4-氧代-7-(4-(2-(4-取代哌嗪-1-基)乙酰基)哌嗪-1-基)喹啉-3-羧酸衍生物作为抗结核和抗菌剂。
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.
机构信息
Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India.
Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, Andhra Pradesh, India.
出版信息
Eur J Med Chem. 2014 Jan;71:324-32. doi: 10.1016/j.ejmech.2013.10.055. Epub 2013 Nov 20.
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 ((1)H NMR, (13)C NMR and LCMS) and screened for their in vitro anti-tubercular and antibacterial activity. Many of these compounds exhibited MIC values in the range 7.32-136.10 μM 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 μM. Compound 3f was found to be the most active with an MIC of 0.44 and 0.8 μM respectively against both the strains. In general, the antibacterial activity of title compounds was more prominent.
合成了一系列 22 种新型 1-环丙基-6-氟-4-氧代-7-(4-取代哌嗪-1-基)-1,4-二氢喹啉-3-羧酸类似物，并对其进行了（1）H NMR、（13）C NMR 和 LCMS 表征以及体外抗结核和抗菌活性筛选。这些化合物中的许多对结核分枝杆菌 H37Rv 的 MIC 值在 7.32-136.10 μM 范围内。进一步对 8 种化合物进行了细胞毒性研究。此外，还对标题化合物进行了抗金黄色葡萄球菌 ATCC 29213（革兰氏阳性）和大肠杆菌 ATCC 25922（革兰氏阴性）细菌的抗菌活性筛选。这些化合物中的许多对金黄色葡萄球菌 ATCC 29213 和大肠杆菌 ATCC 25922 的 MIC 值在 0.44-34.02 μM 范围内。化合物 3f 对两种菌株的 MIC 值分别为 0.44 和 0.8 μM，活性最高。总的来说，标题化合物的抗菌活性更为突出。
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