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通过小分子佐剂增强对传统抗生素的耐药性

Potentiation of Resistance to Conventional Antibiotics through Small Molecule Adjuvants.

作者信息

Stephens Matthew D, Hubble Veroncia B, Ernst Robert K, van Hoek Monique L, Melander Roberta J, Cavanagh John, Melander Christian

机构信息

Department of Chemistry, North Carolina State University, Raleigh, North Carolina 27695, United States.

Department of Microbial Pathogenesis, University of Maryland - Baltimore, Baltimore, MD 21201, United States.

出版信息

Medchemcomm. 2016 Jan 1;7(1):128-131. doi: 10.1039/C5MD00353A. Epub 2015 Sep 30.

DOI:10.1039/C5MD00353A
PMID:26877862
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4749165/
Abstract

A screen of 20 compounds identified small molecule adjuvants capable of potentiating anitbiotic activty against . Analogue synthesis of an initial hit compound led to the discovery of a potentially new class of small molecule adjuvants containg an indole core. The lead compound was able to lower the MIC of colistin by 32-fold against intrinsically resistant .

摘要

对20种化合物进行筛选，确定了能够增强抗生素对……活性的小分子佐剂。对最初筛选出的活性化合物进行类似物合成，发现了一类潜在的含吲哚核心的新型小分子佐剂。该先导化合物能够使黏菌素对固有耐药菌的最低抑菌浓度降低32倍。

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