Department of Chemistry, University of Delhi, Delhi, India.
Arch Pharm (Weinheim). 2012 Nov;345(11):896-901. doi: 10.1002/ardp.201200219. Epub 2012 Sep 4.
A library of unsymmetrical cyclohexane-1,2-diamine derivatives were synthesized and evaluated for their activity against Mycobacterium tuberculosis H37Rv in vitro. Out of the 46 compounds synthesized, eight compounds (11h, 13a, 13e, 13f, 14a, 14c, 14d, and 15d) were found to be active at or below 6.25 µM concentration, with negligible toxicity to human red blood cells at a concentration much higher than the MIC(99) . Compound 13a was the best active compound showing inhibition at 3.125-6.25 µM, and was found to be non-hemolytic up to 500 µg/mL concentration.
合成了一系列非对称环己烷-1,2-二胺衍生物，并评估了它们对结核分枝杆菌 H37Rv 的体外活性。在所合成的 46 种化合物中，有 8 种化合物（11h、13a、13e、13f、14a、14c、14d 和 15d）在 6.25μM 浓度或更低时表现出活性，在远高于 MIC(99)的浓度下对人红细胞几乎没有毒性。化合物 13a 是最具活性的化合物，在 3.125-6.25μM 时表现出抑制作用，且在 500μg/mL 浓度下也没有溶血作用。
