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用于结核分枝杆菌阿拉伯糖基转移酶抑制活性的对称C-连接和假对称O-连接二糖类似物的合成。

Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.

作者信息

Pathak Ashish K, Pathak Vibha, Riordan James R, Suling William J, Gurcha Sudagar S, Besra Gurdyal S, Reynolds Robert C

机构信息

Drug Discovery Division, Southern Research Institute, PO Box 55305, Birmingham, AL 35255, USA.

出版信息

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4527-30. doi: 10.1016/j.bmcl.2007.05.099. Epub 2007 Jun 6.

Abstract

Herein we report the synthesis of symmetrical C-linked and pseudo-symmetrical O-linked disaccharides structurally related to Araf motifs present in the cell wall of MTB. Their activity in a competition-based arabinosyltransferase assay using [14C]-DPA as the glycosyl donor is also presented. In addition, in vitro inhibitory activity for the disaccharides was determined in a colorimetric broth microdilution assay system against MTB H37Ra and Mycobacterium avium.

摘要

在此,我们报告了与结核分枝杆菌细胞壁中存在的阿拉伯糖基(Araf)基序结构相关的对称C-连接和假对称O-连接二糖的合成。还介绍了它们在以[14C]-DPA作为糖基供体的基于竞争的阿拉伯糖基转移酶测定中的活性。此外,在比色肉汤微量稀释测定系统中测定了二糖对结核分枝杆菌H37Ra和鸟分枝杆菌的体外抑制活性。

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