Aurone derivatives as promising antibacterial agents against resistant Gram-positive pathogens.
Antibacterial
Aurones
Bacterial membrane
Gram-positive
MRSA
Resistance
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Mar 2019
01 Mar 2019
Historique:
received:
16
10
2018
revised:
07
01
2019
accepted:
10
01
2019
pubmed:
22
1
2019
medline:
22
3
2019
entrez:
22
1
2019
Statut:
ppublish
Résumé
A set of variously substituted aurones was synthesized and evaluated against Methicillin-Resistant S. aureus (MRSA) and P. aeruginosa. Several analogues were found active against MRSA, but no effect was recorded against P. aeruginosa. Compounds 27, 30 and 33 showed low cytotoxicity, and were tested against a full range of bacterial (Gram-positive and Gram-negative) and fungal species, including resistant strains. These aurones displayed a selective inhibition of Gram-positive bacteria with excellent Therapeutic Index values, while showing no significant action on several Gram-negative strains, H. pylori and V. alginolyticus being the only susceptible strains among the Gram-negative bacteria tested. A permeabilization assay showed that the antibacterial activity of at least some of the aurones could be linked to alterations of the bacterial membrane. Overall, this study endorses the use of the aurone scaffold for the development of new potent and selective antibacterial agents.
Identifiants
pubmed: 30665143
pii: S0223-5234(19)30032-7
doi: 10.1016/j.ejmech.2019.01.022
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Benzofurans
0
aurone
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
133-141Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.