Aurone derivatives as promising antibacterial agents against resistant Gram-positive pathogens
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Elsevier Masson s.r.l.
Abstract
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. © 2019 Elsevier Masson SAS
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Keywords
Antibacterial, Aurones, Bacterial membrane, Gram-positive, Mrsa, Resistance, Anti-bacterial agents, Benzofurans, Cell membrane, Gram-positive bacteria, Methicillin-resistant staphylococcus aureus, Pseudomonas aeruginosa, Structure-activity relationship, 2 (2,4 dimethoxybenzylidene) 4,6 dimethoxybenzofuran 3(2h) one, 2 (3,4 dihydroxybenzylidene) 7 hydroxybenzofuran 3(2h) one, 2 (3,4 dimethoxybenzylidene) 6 methoxybenzofuran 3(2h) one, 2 (4 benzyloxy 3 methoxybenzylidene) 4,6 dihydroxybenzofuran 3(2h) one, 2 benzylidenebenzofuran 3(2h) one, 2 [4 (4 methylpiperazin 1 yl)benzylidene] 6 hydroxybenzofuran 3(2h) one, 6 methoxybenzofuran 3(2h) one, Antibiotic agent, Antifungal agent, Aurone derivative, Unclassified drug, Antiinfective agent, Aurone, Benzofuran derivative, Acinetobacter baumannii, Antibacterial activity, Antibiotic resistance, Antibiotic sensitivity, Antifungal activity, Article, Aspergillus flavus, Aspergillus ochraceus, Bacillus subtilis, Enterococcus, Gram positive bacterium, Helicobacter pylori, Human, Human cell, Klebsiella pneumoniae, Lactococcus lactis, Methicillin resistant staphylococcus aureus, Minimum bactericidal concentration, Minimum inhibitory concentration, Mycobacterium smegmatis, Nonhuman, Peptoclostridium difficile, Propionibacterium acnes, Salmonella enterica, Shigella flexneri, Stachybotrys chartarum, Therapeutic index, Vibrio alginolyticus, Chemistry, Drug effect, Structure activity relation, Ultrastructure