INSA Lyon, ICBMS, Bât J. Verne, 20 av A. Einstein, 69621 Villeurbanne Cedex, France.
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6876-9. doi: 10.1016/j.bmcl.2011.09.010. Epub 2011 Sep 10.
New N-acylhomoserine lactone (AHL) analogues in which the amide function is replaced by a reverse-amide one have been studied as AHL QS modulators. The series of compounds consists of α-(N-alkyl-carboxamide)-γ-butyrolactones, α-(N-alkyl-sulfonamide)-γ-butyrolactones, and 2-(N-alkyl-carboxamide)-cyclopentanones and cyclopentanols. Most active compounds exhibited antagonist activities against LuxR reaching the 30 μM range.
新型 N-酰基高丝氨酸内酯 (AHL) 类似物中,酰胺功能被反向酰胺取代,被用作 AHL QS 调节剂进行研究。该系列化合物包括α-(N-烷基-羧酰胺)-γ-丁内酯、α-(N-烷基-磺酰胺)-γ-丁内酯和 2-(N-烷基-羧酰胺)-环戊酮和环戊醇。大多数活性化合物对 LuxR 表现出拮抗活性,达到 30 μM 范围。