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Synthesis and Evaluation of New Antagonists of Bacterial Quorum Sensing in Vibrio harveyi
Author(s) -
Peng Hanjing,
Cheng Yunfeng,
Ni Nanting,
Li Minyong,
Choudhary Gaurav,
Chou Han Ting,
Lu ChungDar,
Tai Phang C.,
Wang Binghe
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900180
Subject(s) - vibrio harveyi , quorum sensing , biofilm , autoinducer , microbiology and biotechnology , organism , biology , chemistry , model organism , minimum inhibitory concentration , bacteria , computational biology , vibrio , biochemistry , gene , antimicrobial , genetics
Bacterial quorum sensing has received much attention in recent years because of its relevance to pathological events such as biofilm formation. Based on the structures of two lead inhibitors (IC 50 : 35–55 μ M ) against autoinducer‐2‐mediated quorum sensing identified through virtual screening, we synthesized 39 analogues and examined their inhibitory activities. Twelve of these new analogues showed equal or better inhibitory activities than the lead inhibitors. The best compound showed an IC 50 value of ∼6 μ M in a whole‐cell assay using Vibrio harveyi as the model organism. The structure–activity relationship is discussed herein.