Minvielle Marine J, Bunders Cynthia A, Melander Christian
Department of Chemistry, North Carolina State University, Raleigh, NC, 27695-8204, USA. ; Tel: +1 919-513-2960.
Medchemcomm. 2013 Jun 1;4(6):916-919. doi: 10.1039/C3MD00064H.
Herein is described a method of accessing indole/triazole and benzothiophene/triazole analogues that selectively promote or inhibit biofilm formation by Gram-positive and Gram-negative bacteria. Structure/function studies revealed that the addition of a bromine atom at the 2-position of the indole/triazole scaffold altered activity against both Gram-negative and Gram-positive bacteria and could transform a biofilm inhibitor into a biofilm inducer. Isosteric replacement of the indole core by a benzothiophene significantly impaired anti-biofilm activity. A competition assay exposing to the most potent biofilm inducer and an inhibitor of biofilm formation was performed. The inducer exhibited the ability to mute the effect of the anti-biofilm compound for this targeted bacterial population.
本文描述了一种获取吲哚/三唑和苯并噻吩/三唑类似物的方法，这些类似物可选择性地促进或抑制革兰氏阳性菌和革兰氏阴性菌的生物膜形成。结构/功能研究表明，在吲哚/三唑支架的2位添加溴原子会改变对革兰氏阴性菌和革兰氏阳性菌的活性，并可将生物膜抑制剂转化为生物膜诱导剂。用苯并噻吩对吲哚核心进行等排取代会显著损害抗生物膜活性。进行了一项竞争试验，将其暴露于最有效的生物膜诱导剂和生物膜形成抑制剂中。对于该目标细菌群体，诱导剂表现出使抗生物膜化合物的作用失效的能力。
