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含硼肽模拟物——一类新型选择性抗结核药物。

Boron-containing peptidomimetics--a novel class of selective anti-tubercular drugs.

机构信息

Department of Chemistry, University of Tromsø, N-9037 Tromsø, Norway.

出版信息

Chem Biol Drug Des. 2013 Mar;81(3):408-13. doi: 10.1111/cbdd.12091. Epub 2012 Dec 26.

Abstract

Medical treatment for tuberculosis is complicated nowadays by the appearance of new multiresistant strains, and therefore, new antibiotics are in great need. Here, we report the synthesis and in vitro testing of a new class of highly selective antimicrobial boron-containing peptidomimetics with compounds exhibiting activity against Mycobacterium tuberculosis at ≤5 μg/mL. The new approach developed makes it possible to synthesize variously substituted β-aminoboronic acids and their derivatives with a high level of diastereoselectivity.

摘要

目前,新的耐多药菌株的出现使结核病的治疗变得复杂,因此急需新型抗生素。在此,我们报告了一类新型高选择性含硼抗菌肽模拟物的合成和体外测试,其中一些化合物对结核分枝杆菌的活性可低至 5 μg/mL。所开发的新方法使得能够高立体选择性地合成各种取代的β-氨基硼酸及其衍生物。

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