抗分枝杆菌剂。1. 嘌呤的硫类似物。
Antimycobacterial agents. 1. Thio analogues of purine.
作者信息
Pathak Ashish K, Pathak Vibha, Seitz Lainne E, Suling William J, Reynolds Robert C
机构信息
Drug Discovery Division, Southern Research Institute, P.O. Box 55305, Birmingham, Alabama 35255-5305, USA.
出版信息
J Med Chem. 2004 Jan 1;47(1):273-6. doi: 10.1021/jm030389b.
Thio analogues of purine, pyridine, and pyrimidine were prepared based on the initial activity screening of several analogues of these heterocycles against Mycobacterium tuberculosis (Mtb). Certain 6-thio-substituted purine analogues described herein showed moderate to good inhibitory activity. In particular, two purine analogues 9-(ethylcarboxymethyl)-6-(decylthio)-9H-purine (20) and 9-(ethylcarboxymethyl)-6-(dodecylthio)-9H-purine (21) exhibited MIC values of 1.56 and 0.78 microg/mL respectively against the Mtb H(37)Rv strain. N(9)-Substitution apparently enhances the antimycobacterial activity in the purine series described herein.
基于对这些杂环化合物的几种类似物针对结核分枝杆菌（Mtb）的初步活性筛选，制备了嘌呤、吡啶和嘧啶的硫代类似物。本文所述的某些6-硫代取代嘌呤类似物表现出中等至良好的抑制活性。特别地，两种嘌呤类似物9-(乙基羧甲基)-6-(癸硫基)-9H-嘌呤（20）和9-(乙基羧甲基)-6-(十二烷基硫基)-9H-嘌呤（21）对Mtb H(37)Rv菌株的MIC值分别为1.56和0.78μg/mL。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。
Zotero 插件