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Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2019

Aurone derivatives as promising antibacterial agents against resistant Gram-positive pathogens

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 per-meabilization 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.
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hal-01988325 , version 1 (21-10-2021)

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Paternité - Pas d'utilisation commerciale

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Hamza Olleik, Samir Yahiaoui, Brayan Roulier, Elise Courvoisier-Dezord, Josette Perrier, et al.. Aurone derivatives as promising antibacterial agents against resistant Gram-positive pathogens. European Journal of Medicinal Chemistry, 2019, 165, pp.133-141. ⟨10.1016/j.ejmech.2019.01.022⟩. ⟨hal-01988325⟩
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