作为潜在抗结核药物的环取代喹啉
Ring-substituted quinolines as potential anti-tuberculosis agents.
作者信息
Vangapandu Suryanarayana, Jain Meenakshi, Jain Rahul, Kaur Sukhraj, Singh Prati Pal
机构信息
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
出版信息
Bioorg Med Chem. 2004 May 15;12(10):2501-8. doi: 10.1016/j.bmc.2004.03.045.
We report in vitro antimycobacterial properties of ring-substituted quinolines (series 1-4) constituting 56 analogues against drug-sensitive and drug-resistant M. tuberculosis H37Rv strains. The most effective compounds 2h (R1 = R2 = c-C6H11, R3 = NO2, series 1) and 13g (R1 = OC7H15, R2 = NO2, series 4) have exhibited an MIC value of 1 microg/mL against drug-sensitive M. tuberculosis H37Rv strain that is comparable to first line anti-tuberculosis drug, isoniazid. Selected analogues (2d, 2g, 2h, 4e, 6b, 13b, 13g, and 14e, MIC: < or = 6.25 microg/mL) upon further evaluation against single-drug-resistant (SDR) strains of M. tuberculosis H37Rv have produced potent efficacy in the range between 6.25 and 50 microg/mL.
我们报告了由56个类似物组成的环取代喹啉（系列1 - 4）对药物敏感和耐药的结核分枝杆菌H37Rv菌株的体外抗分枝杆菌特性。最有效的化合物2h（R1 = R2 = 环戊基，R3 = NO2，系列1）和13g（R1 = OC7H15，R2 = NO2，系列4）对药物敏感的结核分枝杆菌H37Rv菌株的最低抑菌浓度（MIC）值为1微克/毫升，与一线抗结核药物异烟肼相当。对结核分枝杆菌H37Rv的单药耐药（SDR）菌株进一步评估后，选定的类似物（2d、2g、2h、4e、6b、13b、13g和14e，MIC：≤6.25微克/毫升）在6.25至50微克/毫升的范围内产生了强效效果。
Zotero 插件