Discovery of Novel Tetrazoles Featuring a Pyrazole Moiety as Potent and Highly Selective Antifungal Agents.

ABSTRACT: In pursuit of developing novel azole antifungals with potent activity and high selectivity, a series of (2R,3S)-3-(substituted-1H-pyrazol-3-yl)-2-(2,4-difluorophenyl)-1-(1H-tetrazol-1-yl)butan-2-ol derivatives were designed and synthesized based on our previous work. All compounds exhibited excellent in vitro antifungal activities against Candida spp. and Cryptococcus neoformans H99 with minimum inhibitory concentration values ranging from <0.008 to 4 μg/mL, with some even showing moderate activity against Aspergillus fumigatus 7544. The most active compounds (8, 11, 15, 24, and 25) displayed outstanding antifungal activity against six fluconazole-resistant C. auris clinical isolates and showe

SUBMITTER: Chi X 

PROVIDER: S-EPMC10193422 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature