Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

Park, Suzie; Kim, Han-Shin; Ok, Kiwon; Kim, YunHye; Park, Hee-Deung; Byun, Youngjoo

doi:10.1016/j.bmcl.2015.05.054

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Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

Park, Suzie;
Kim, Han-Shin;
Ok, Kiwon;
Kim, YunHye;
Park, Hee-Deung;
... Byun, Youngjoo

Citations

WEB OF SCIENCE

45

Citations

SCOPUS

48

초록

Novel pyrone-derived quorum sensing (QS) ligands to inhibit the binding of OdDHL to the LasR of Pseudomonas aeruginosa were designed, synthesized and evaluated. Among the analogs, the most potent compound 8 exhibited strong in vitro inhibitory activities against biofilm formation and down-regulated OdDHL/LasR-associated genes by 35-67%. The binding mode of 8 in silico was highly similar to that of the crystal ligand OdDHL in the active site of LasR. (C) 2015 Elsevier Ltd. All rights reserved.

키워드

Quorum sensing; Biofilm inhibition; Pyrone; Pseudomonas aeruginosa; PSEUDOMONAS-AERUGINOSA VIRULENCE; ACYL HOMOSERINE LACTONES; RATIONAL DESIGN; MODULATORS; BIOFILM; TRIAZOLE; ANALOGS; AUTOINDUCER; INFECTIONS; BACTERIA

제목: Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

저자: Park, Suzie; Kim, Han-Shin; Ok, Kiwon; Kim, YunHye; Park, Hee-Deung; Byun, Youngjoo

DOI: 10.1016/j.bmcl.2015.05.054

발행일: 2015-08-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 25

호: 15

페이지: 2913 ~ 2917

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 5 페이지

ISSN: E 1464-3405
P 0960-894X