Rational Design of New Monoterpene-Containing Azoles and Their Antifungal Activity.

ABSTRACT: Azole antifungals, including fluconazole, have long been the first-line antifungal agents in the fight against fungal infections. The emergence of drug-resistant strains and the associated increase in mortality from systemic mycoses has prompted the development of new agents based on azoles. We reported a synthesis of novel monoterpene-containing azoles with high antifungal activity and low cytotoxicity. These hybrids demonstrated broad-spectrum activity against all tested fungal strains, with excellent minimum inhibitory concentration (MIC) values against both fluconazole-susceptible and fluconazole-resistant strains of Candida spp. Compounds 10a and 10c with cuminyl and pinenyl fragments demonstrated up to 100 times lower MICs than fluconazole against clinical isolat

SUBMITTER: Li-Zhulanov NS 

PROVIDER: S-EPMC10215469 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature