Bioorganic & medicinal chemistry · 2025
Halogenated N-(1,3,4-oxadiazol-2-yl) benzamides are effective eradicators of methicillin-resistant Staphylococcus aureus biofilms.
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Naclerio George A, Vennard Christopher S, Onyedibe Kenneth I, Vieira Dielson da S, Abutaleb Nader S, Figueiredo Marxa L, Seleem Mohamed N, Sintim Herman O
Аннотация
Due to the ever-increasing threat of methicillin-resistant Staphylococcus aureus (MRSA), we have embarked on a campaign to discover novel antibacterial agents which are effective at eradicating both MRSA, as well as acting on pre-formed MRSA biofilms. Using the known scaffold of N-(1,3,4-oxadiazol-2-yl)benzamides, we performed a halogenation study which has led to the identification of HSGN-2241. This novel compound was found to effectively kill many multi-drug resistant Gram-positive clinical isolates in a bactericidal manner. The growth inhibition mechanism of HSGN-2241 was found to be via potassium ion release and subsequent depolarization of the cell membrane. As an initial safety test, HSGN-2241 was found to not lyse human red blood cells, so it is a promising lead compound for the treatment of bacterial infections caused by Staphylococcus aureus.