Antifungal agent 25

Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo[1].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Fungal

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].

Antifungal agent 25 (2 mg/kg; i.v.) exhibits stable metabolic property in SD rats[1]. Pharmacokinetic Parameters of Antifungal agent 25 in SD rats[1]. dose(mg/kg) C0(ng/mL) T1/2(h) Vdss(L/kg) Cl (mL/min/kg) AUC0-last (ng·h/mL) AUC0-inf (ng·h/mL) 2 mg/kg 482±108 3.34±2.37 10.3±3.12 69.4±18.8 483±137 5.5±136SD rats; 2 mg/kg; i.v.[1]. Animal Model: SD rats[1] Dosage: 2 mg/kg Administration: I.v. Result: Exhibited stable metabolic property in SD rats.

[1]. Zhao L, et al. Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents. Eur J Med Chem. 2022; 228:113987.