Design, Synthesis, and In Vitro and In Vivo Antifungal Activity of Novel Triazoles Containing Phenylethynyl Pyrazole Side Chains.

A series of triazole derivatives containing phenylethynyl pyrazole moiety as side chain were designed, synthesized, and most of them exhibited good in vitro antifungal activities. Especially, compounds and showed excellent in vitro activities against (MIC = 0.125, 0.0625 μg/mL), (MIC = 0.125, 0.0625 μg/mL), and (MIC = 8.0, 4.0 μg/mL). Compound also exerted superior activity to compound and fluconazole in inhibiting hyphae growth of and inhibiting drug-resistant strains of , and it could reduce fungal burdens in mice kidney at a dosage of 1.0 mg/kg. An in vivo efficacy evaluation indicated that could effectively protect mice models from infection at doses of 0.5, 1.0, and 2.0 mg/kg. These results suggested that compound deserves further investigation.