Anthem Biosciences Pvt Ltd, 49 Bommasandra Industrial Area, Bommasandra, Bangalore 560 099, Karnataka, India.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1040-4. doi: 10.1016/j.bmcl.2009.12.045. Epub 2009 Dec 16.
A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC(2)), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis.
已经合成了一系列带有活性药效团的 26 种新型喹啉衍生物,并通过肉汤微量稀释法评估了它们对结核分枝杆菌 H37Rv(MTB)、耻垢分枝杆菌(MC(2))和偶然分枝杆菌的体外抗结核活性。与一线药物异烟肼(INH)和利福平(RIF)相比,化合物 13e、13i、13k、14a、14c、14i 和 14k 表现出显著的最低抑制浓度,并且可以进一步进行修饰,以获得更有效的化合物来对抗耐多药结核病。