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新型糖衍生物的合成及其对结核分枝杆菌的抗菌活性评价。

Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.

机构信息

Department of Molecular Health Sciences, Graduate School of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.

出版信息

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6313-6. doi: 10.1016/j.bmcl.2009.09.095. Epub 2009 Sep 27.

Abstract

A series of sugar derivatives (1-13) were synthesized and evaluated for antibacterial activity against Mycobacteriumtuberculosis (MTB), especially multi-drug resistant (MDR) MTB, and the structure-activity relationships of these compounds were studied. The results showed that the compound OCT313 (2-acetamido-2deoxy-beta-D-glucopyranosyl N,N-dimethyldithiocarbamate) (4) exhibited significant in vitro bactericidal activity, and that the dithiocarbamate group at C-1 position of the glucopyranoside ring was requisite for the antibacterial activity.

摘要

一系列糖衍生物(1-13)被合成并评估了对结核分枝杆菌(MTB),特别是耐多药 MTB 的抗菌活性,并且研究了这些化合物的构效关系。结果表明,化合物 OCT313(2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖基 N,N-二甲基二硫代氨基甲酸盐)(4)表现出显著的体外杀菌活性,并且吡喃葡萄糖环 C-1 位的二硫代氨基甲酸盐基团是抗菌活性所必需的。

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