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Discovery and Characterization of Pure RhIR Antagonists against Pseudomonas aeruginosa Infections

Authors
Nam, SangJinHam, So-YoungKwon, HongmokKim, Han-ShinMoon, SuhyunLee, Jeong-HoonLim, TaehyeongSon, Sang-HyunPark, Hee-DeungByun, Youngjoo
Issue Date
Aug-2020
Publisher
American Chemical Society
Citation
Journal of Medicinal Chemistry, v.63, no.15, pp 8388 - 8407
Pages
20
Indexed
SCIE
SCOPUS
Journal Title
Journal of Medicinal Chemistry
Volume
63
Number
15
Start Page
8388
End Page
8407
URI
https://scholarworks.korea.ac.kr/kumedicine/handle/2020.sw.kumedicine/33648
DOI
10.1021/acs.jmedchem.0c00630
ISSN
0022-2623
Abstract
Pseudomonas aeruginosa (P. aeruginosa) is an opportunistic human pathogen that forms biofilms and produces virulence factors via quorum sensing (QS). Blocking the QS system in P. aeruginosa is an excellent strategy to reduce biofilm formation and the production of virulence factors. RhIR plays an essential role in the QS system of P. aeruginosa. We synthesized 55 analogues based on the chemical structure of 4-gingerol and evaluated their RhIR inhibitory activities using the cell-based reporter strain assay. Comprehensive structure-activity relationship studies identified the alkynyl ketone 30 as the most potent RhIR antagonist. This compound displayed selective RhIR antagonism over LasR and PqsR, strong inhibition of biofilm formation, and reduced production of virulence factors in P. aeruginosa. Furthermore, the survival rate of Tenebrio molitor larvae treated with 30 in 30, a pure RhIR antagonist, can be utilized for developing QS-modulating molecules vivo greatly improved. Therefore, compound in the control of P. aeruginosa infections.
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