Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents. (6th March 2017)

• Record Type: Journal Article
• Authors: Zhou, Ziteng; Ma, Shutao
• Is Part Of: ChemMedChem. Volume 12:Number 6(2017)
• Page Start: 420
• Page End: 425
• Publication Date: 2017-03-06
• Subjects: antimicrobial agents -- inhibitors -- PqsD -- quinolone signal -- quorum sensing; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201700015
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: The treatment of the infections caused by Pseudomonas aeruginosa, an opportunistic Gram‐negative bacterium, is very difficult. High intrinsic tolerance toward common antibiotics and the development of new resistant strains challenge us to find a new treatment as soon as possible. PqsD is an enzyme essential for the P. aeruginosa quorum‐sensing apparatus, which catalyzes the final and key step in the biosynthesis of 4‐hydroxy‐2‐heptylquinolone (HHQ), which is a signal molecule of the P. aeruginosa quorum‐sensing system. In this review, following an outline on their structures, we present a brief introduction of the PqsD inhibitors including their mechanisms of action, inhibitory activity, and structure–activity relationships. Abstract : Scrambling their signals : Antibiotic resistance is a growing threat to public health. Recently, anti‐quorum sensing (QS) has been recognized as an attractive strategy in the fight against bacteria based on antivirulence and antibiofilm action, and not on bacterial killing. The target protein PqsD is a key player in the quorum‐sensing system of Pseudomonas aeruginosa . This review highlights recent advances in the search for new synthetic PqsD inhibitors, focusing on their biological activity, selectivity, and structure–activity relationship information.