Citation: Bao Gang Wang, Shi Chong Yu, Xiao Yun Chai, Yong Zheng Yan, Hong Gang Hu, Qiu Ye Wu. Design synthesis and biological evaluation of 3-substituted triazole derivatives[J]. Chinese Chemical Letters, ;2011, 22(5): 519-522. doi: 10.1016/j.cclet.2010.11.029 shu

Design synthesis and biological evaluation of 3-substituted triazole derivatives

a Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;
b Pharmacy Team, Administrative Brigade of Postgraduate, Second Military Medical University, Shanghai 200433, China

Received Date: 23 August 2010

Fund Project: This work was supported by the National Natural Science Foundation of China (No.20772153)Shanghai Leading Academic Discipline Project(No.B906)and by Creativity and Innovation Training Program of Second Military Medical University (No.MS2009042)

Based on the active site of lanosterol 14α-demethylase of azole antifungal agents, sixteen l-(lH-l,2,4-triazole-l-yl)-2-(2,4-difluorophenyl)-3-(N-n-butyl-N-l-substitutedbenzyl-4-methylene-lH-l,2,3-triazole)-2-propanols have been designed, synthesized and evaluated as antifungal agents.Results of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that some of the compounds exhibited excellent activities with broad spectrum.
- Synthesis,
- Triazole,
- Antifungal activity,
- 1,3-Dipolar cycloaddition
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