European Journal of Medicinal Chemistry p. 96 - 107 (2017)
Update date:2022-08-30
Topics:
Zhao, Shizhen
Zhang, Xiangqian
Wei, Peng
Su, Xin
Zhao, Liyu
Wu, Mengya
Hao, Chenzhou
Liu, Chunchi
Zhao, Dongmei
Cheng, Maosheng
To further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (1), a series of aromatic heterocyclic derivatives were designed, synthesized and evaluated for in vitro antifungal activity. Many of the target compounds showed good inhibitory activity against Candida albicans and Cryptococcus neoformans. In particular, the isoxazole nuclei were more suited for improving the activity against Aspergillus spp. Among these compounds, 2-F substituted analogues 23g and 23h displayed the most remarkable in vitro activity against Candida spp., C. neoformans, A. fumigatus and fluconazole-resistant C.alb. strains, which is superior or comparable to the activity of the reference drugs fluconazole and voriconazole. Notably, the compounds 23g and 23h exhibited low inhibition profiles for various isoforms of human cytochrome P450 and excellent blood plasma stability.
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