Thioether-linked dihydropyrrol-2-one analogues as PqsR antagonists against antibiotic resistant Pseudomonas aeruginosa.

Anti-Bacterial Agents / chemical synthesis Dose-Response Relationship, Drug Drug Resistance, Bacterial / drug effects Microbial Sensitivity Tests Molecular Structure Pseudomonas aeruginosa / drug effects Pyrroles / chemistry Quorum Sensing / drug effects Structure-Activity Relationship Sulfides / chemistry
Dihydropyrrol-2-one (DHP) analogues PqsR antagonist Pseudomonas aeruginosa Pseudomonas quinolone system Quorum sensing inhibitors

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 02 2021
Historique:
received: 18 10 2020
revised: 15 12 2020
accepted: 18 12 2020
pubmed: 13 1 2021
medline: 1 9 2021
entrez: 12 1 2021
Statut: ppublish

Résumé

The Pseudomonas quinolone system (pqs) is one of the key quorum sensing systems in antibiotic-resistant P. aeruginosa and is responsible for the production of virulence factors and biofilm formation. Thus, synthetic small molecules that can target the PqsR (MvfR) receptor can be utilized as quorum sensing inhibitors to treat P. aeruginosa infections. In this study, we report the synthesis of novel thioether-linked dihydropyrrol-2-one (DHP) analogues as PqsR antagonists. Compound 7g containing a 2-mercaptopyridyl linkage effectively inhibited the pqs system with an IC

Identifiants

DOI: 10.1016/j.bmc.2020.115967 PMID: 33434766
pubmed: 33434766
pii: S0968-0896(20)30797-5
doi: 10.1016/j.bmc.2020.115967
pii:
doi:

Substances chimiques

Anti-Bacterial Agents 0
Pyrroles 0
Sulfides 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

115967

Informations de copyright

Copyright © 2020 Elsevier Ltd. All rights reserved.

Auteurs

Shekh Sabir (S)

School of Chemistry, The University of New South Wales, NSW 2052 Sydney, Australia. Electronic address: s.sabir@student.unsw.edu.au.

Dittu Suresh (D)

School of Chemistry, The University of New South Wales, NSW 2052 Sydney, Australia.

Sujatha Subramoni (S)

Singapore Centre for Environmental Life Sciences Engineering (SCELSE), Nanyang Technological University, 637551 Singapore, Singapore. Electronic address: subramoni@ntu.edu.sg.

Theerthankar Das (T)

Department of Infectious Diseases and Immunology, School of Medical Sciences, The University of Sydney, NSW 2006 Sydney, Australia. Electronic address: das.ashishkumar@sydney.edu.au.

Mohan Bhadbhade (M)

Mark Wainwright Analytical Centre, UNSW Sydney, Australia. Electronic address: m.bhadbhade@unsw.edu.au.

David StC Black (DS)

School of Chemistry, The University of New South Wales, NSW 2052 Sydney, Australia. Electronic address: d.black@unsw.edu.au.

Scott A Rice (SA)

Singapore Centre for Environmental Life Sciences Engineering (SCELSE), Nanyang Technological University, 637551 Singapore, Singapore. Electronic address: rscott@ntu.edu.sg.

Naresh Kumar (N)

School of Chemistry, The University of New South Wales, NSW 2052 Sydney, Australia. Electronic address: n.kumar@unsw.edu.au.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Résistance aux substances › Résistance microbienne aux médicaments › Résistance bactérienne aux médicaments › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Bactéries › Proteobacteria › Gammaproteobacteria › Pseudomonadaceae › Pseudomonas › Pseudomonas aeruginosa › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Pyrroles › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Phénomènes microbiologiques › Interactions microbiennes › Détection du quorum › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Thioether-linked dihydropyrrol-2-one analogues...
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Sulfures › Thioether-linked dihydropyrrol-2-one analogues...