Synthesis and evaluation of new antagonists of bacterial quorum sensing in Vibrio harveyi

Hanjing Peng, Yunfeng Cheng, Nanting Ni, Minyong Li, Gaurav Choudhary, Han Ting Chou, Chung Dar Lu, Phang C. Tai, Binghe Wang

Research output: Contribution to journalArticle

Abstract

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 (IC50 : 35-55 μM) 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 IC50 value of ∼6 μm in a whole-cell assay using Vibrio harveyi as the model organism. The structure-activity relationship is discussed herein.

Original languageEnglish (US)
Pages (from-to)1457-1468
Number of pages12
JournalChemMedChem
Volume4
Issue number9
DOIs
StatePublished - Sep 4 2009
Externally publishedYes

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Keywords

  • Autoinducer-2
  • CoMFA
  • Drug design
  • Inhibitors
  • Quorum sensing

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

Peng, H., Cheng, Y., Ni, N., Li, M., Choudhary, G., Chou, H. T., Lu, C. D., Tai, P. C., & Wang, B. (2009). Synthesis and evaluation of new antagonists of bacterial quorum sensing in Vibrio harveyi. ChemMedChem, 4(9), 1457-1468. https://doi.org/10.1002/cmdc.200900180