In Vitro |
Antifungal agent 25 (compound A31) shows antifungal effect with MIC values of <0.03, <0.03, <0.03, 0.25, 0.5 µg/mL for Candida albicans (SC5314), Candida albicans ((GIM 2.194), Cryptococcus neoformans (GIM 2.209), Candida tropicalis (GIM 2.183), Aspergillus fumigatus (cgmcc 3.7795), respectively[1]. Antifungal agent 25 shows moderate antifungal activity with MIC values of 0.5, >64 µg/mL for strain CaR (fluconazole-resistant strain of Candida albicans) and strain 17# (fluconazole and itraconazole resistant strain of Candida albicans), respectively[1]. Antifungal agent 25 (0.015 mg/mL) blocks the biosynthesis of ergosterol by inhibiting the key enzyme lanosterol 14a-demethylase (CYP51)[1]. Antifungal agent 25 shows less likely to produce drug-drug interactions with IC50s of 4.47, 2.87, 1.04, 31.3, 10.1 µM for α-naphthoflavone (CYP1A2), sulfaphenazole (CYP2C9), ticlopidine (CYP2C19), quinidine (CYP2D6), and ketoconazole (CYP3A4), respectively[1].
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