Exploration of Baicalein-Core Derivatives as Potent Antifungal Agents: SAR and Mechanism Insights.

ABSTRACT: Baicalein (BE), the major component of Scutellaria Baicalensis, exhibited potently antifungal activity against drug-resistant Candida albicans, and strong inhibition on biofilm formation. Therefore, a series of baicalein-core derivatives were designed and synthesized to find more potent compounds and investigate structure-activity relationship (SAR) and mode of action (MoA). Results demonstrate that A4 and B5 exert a more potent antifungal effect (MIC₈₀ = 0.125 μg/mL) than BE (MIC₈₀ = 4 μg/mL) when used in combination with fluconazole (FLC), while the MIC₈₀ of FLC dropped from 128 μg/mL to 1 μg/mL. SAR analysis indicates that the presence of 5-OH is crucial for synergistic antifungal activities, while o-dihyd

SUBMITTER: Zhou H 

PROVIDER: S-EPMC10489750 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature