Isothiazolone-Nitroxide Hybrids with Activity against Antibiotic-Resistant Staphylococcus aureus Biofilms.

ABSTRACT: Isothiazolones are widely used as biocides in industrial processing systems and personal care products, but their use to treat infections in humans has been hampered by their inherent cytotoxicity. Herein, we report a strategy to alleviate isothiazolone toxicity and improve antibacterial and antibiofilm potency by functionalization with a nitroxide moiety. Isothiazolone-nitroxide hybrids 6 and 22 were prepared over three steps in moderate yields (58 and 36%, respectively) from (Z)-3-(benzylsulfanyl)-propenoic acid. Hybrid 22 displayed better activity (minimum inhibitory concentration (MIC) = 35 μM) than the widely used methylisothiazolinone (MIT 1, MIC = 280 μM) against methicillin-susceptible Staphylococcus aureus (MSSA). Hybrid 22 was even

SUBMITTER: Verderosa AD 

PROVIDER: S-EPMC8851655 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature