6-氧代和 6-硫嘌呤类似物作为抗分枝杆菌剂。
6-Oxo and 6-thio purine analogs as antimycobacterial agents.
机构信息
Drug Discovery Division, Southern Research Institute, 2000 9th Avenue South, Birmingham, AL 35205, USA.
出版信息
Bioorg Med Chem. 2013 Apr 1;21(7):1685-95. doi: 10.1016/j.bmc.2013.01.054. Epub 2013 Feb 4.
Abstract
6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N(9)-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb.
摘要
基于对一个小型多样的嘌呤文库针对结核分枝杆菌（Mtb）的初始活性筛选，制备了 6-氧代和 6-硫代嘌呤类似物。本文所述的某些 6-氧代和 6-硫代取代嘌呤类似物表现出中等至良好的抑制活性。N（9）取代显然增强了本文所述嘌呤系列中的抗分枝杆菌活性。还合成了几种 2-氨基和 2-氯嘌呤类似物，它们对 Mtb 表现出中等抑制活性。
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