Citation: Zhi Gang Dan, Jun Zhang, Shi Chong Yu, Hong Gang Hu, Xiao Yun Chai, Qing Yan Sun, Qiu Ye Wu. Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase (CYP51)[J]. Chinese Chemical Letters, ;2009, 20(8): 935-938. doi: 10.1016/j.cclet.2009.03.027 shu

Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase (CYP51)

Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 22 December 2008

Fund Project: This work was supported by the National Natural Science Foundation of China (No.20772153) and by Shanghai Leading Academic Discipline Project (No.B906).

A series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase (CYP51). Their structures were confirmed by MS and ¹H NMR. In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi. The results showed that all title compounds exhibited activity against fungi tested to some extent. Compounds 3c, 3d, 7a, 7b and 7c exhibited more potent antifungal activities against nearly all fungi tested except Aspergillus fumigatus than fluconazole.
- Triazole,
- Synthesis,
- Antifungal activity
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