title: Recent Advances in the Discovery of PqsD Inhibitors as Antimicrobial Agents.
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.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan, 250012, PR China).
authors.forename: Ziteng
authors.initials: Z
authors.lastname: Zhou
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan, 250012, PR China).
authors.forename: Shutao
authors.initials: S
authors.lastname: Ma
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D002264:Carboxylic Acids / Q000737:chemistry / Q000494:pharmacology; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000378:metabolism; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology; D053038:Quorum Sensing / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D001426:Bacterial Proteins; D001565:Benzoates; D002264:Carboxylic Acids; D015363:Quinolones
keywords: PqsD; antimicrobial agents; inhibitors; quinolone signal; quorum sensing