结核分枝杆菌中硫醇-S-共轭酰胺酶底物模拟抑制剂的设计与合成
Design and synthesis of substrate-mimic inhibitors of mycothiol-S-conjugate amidase from Mycobacterium tuberculosis.
作者信息
Metaferia Belhu B, Ray Satyajit, Smith Jeremy A, Bewley Carole A
机构信息
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jan 15;17(2):444-7. doi: 10.1016/j.bmcl.2006.10.031. Epub 2006 Oct 17.
The Staudinger reaction between a polymer-supported triphenylphosphine reagent and pseudo-disaccharide azides is successfully applied to synthesize a variety of substrate-mimic mycothiol analogs. Screening of this new group of analogs against the mycobacterial detoxification enzyme mycothiol-S-conjugate amidase (MCA) yielded several modest inhibitors (IC50 values around 50 microM) and provided additional structure-activity relationships for future optimization of inhibitors of MCA and its homologs.
聚合物负载的三苯基膦试剂与假二糖叠氮化物之间的施陶丁格反应成功应用于合成多种模拟底物的巯基乙胺酸类似物。对这组新类似物针对分枝杆菌解毒酶巯基乙胺酸-S-共轭酰胺酶（MCA）进行筛选，得到了几种中等强度的抑制剂（IC50值约为50 microM），并为未来优化MCA及其同源物的抑制剂提供了更多的构效关系。
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