设计、3-(9H-芴-9-基)吡咯烷-2,5-二酮衍生物的化学合成及对烯酰基辅酶 A 还原酶（InhA）和结核分枝杆菌的生物活性。
Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.
机构信息
CNRS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, UMR-5068, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France; Université de Toulouse, UPS, Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, LSPCMIB, 118 Route de Narbonne, F-31062 Toulouse Cedex 9, France; Taras Shevchenko National University of Kyiv, Department of Chemistry, 64 Str. Volodymyrska, Kyiv 01033, Ukraine.
出版信息
Eur J Med Chem. 2013;70:37-48. doi: 10.1016/j.ejmech.2013.09.041. Epub 2013 Oct 2.
We report here the discovery, synthesis and screening results of a series of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives as a novel class of potent inhibitors of Mycobacterium tuberculosis H37Rv strain as well as the enoyl acyl carrier protein reductase (ENR) InhA. Among them, several compounds displayed good activities against InhA which is one of the key enzymes involved in the type II fatty acid biosynthesis pathway of the mycobacteria cell wall. Furthermore, some exhibited promising activities against M. tuberculosis and multi-drug resistant M. tuberculosis strains.
我们在此报告了一系列 3-(9H-芴-9-基)吡咯烷-2,5-二酮衍生物的发现、合成和筛选结果，它们是新型强效分枝杆菌 H37Rv 菌株以及烯酰基辅酶 A 还原酶 (ENR) InhA 的抑制剂。其中，一些化合物对 InhA 表现出良好的活性，InhA 是分枝杆菌细胞壁中 II 型脂肪酸生物合成途径的关键酶之一。此外，一些化合物对结核分枝杆菌和耐多药结核分枝杆菌菌株表现出有希望的活性。
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