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Design, synthesis and antibacterial evaluation of novel AHL analogues

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
23
Issue
14
Identifiers
DOI: 10.1016/j.bmcl.2013.05.035
Keywords
  • Antibacterial
  • Quorum Sensing
  • Dithiocarbamates
  • Ahls
Disciplines
  • Design

Abstract

Abstract Two series of novel AHL analogues were designed, synthesized and evaluated for antibacterial activity under cell membrane conditions in vitro. Analogues 4a–c and 4g–m presented potent activity against Gram-positive bacteria. Especially the analogue 4l exerted the most potent inhibition against Bacillus subtilis with MIC50 value of 1.443μg/ml. To our surprise, analogues 6a–c and 6g showed weak inhibition against Gram-negative bacteria with MIC50 values ranging from 17.589 to 67.840μg/ml. This was the first report about synthesis and antibacterial evaluation in vitro of AHL analogues containing dithioester linkage.

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