Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity
Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity
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DOI：
10.1016/j.bmcl.2015.02.023
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发表时间：
2015-04-15
影响因子：
2.7
通讯作者：
Xu, Zhi-Bin
中科院分区：
文献类型：
--
作者：
Dong, Ying-Jie;Meng, Zi-Hui;Xu, Zhi-Bin
结核病（TB）的全球威胁导致了对新药的巨大需求，特别是那些可以治疗耐多药结核病的新药。我们合成了新的截短侧耳素衍生物与N-苄胺侧链取代的C14位，并评估其活性在体外对结核分枝杆菌的强毒株（H37Rv）。初步测定结果显示，五种化合物在20 μ M时抑制H37 Rv，其中一种类似物的MIC低至7.2 μ M。(C)2015爱思唯尔有限公司版权所有。
The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 mu M, with a MIC of one of the analogues as low as 7.2 mu M. (C) 2015 Elsevier Ltd. All rights reserved.