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

作　　者：Zhi Gang Dan Jun Zhang Shi Chong Yu Hong Gang Hu Xiao Yun Chai Qing Yan Sun Qiu Ye Wu 

机构地区：[1]Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

出　　处：《Chinese Chemical Letters》2009年第8期935-938,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.20772153);by Shanghai Leading Academic Discipline Project(No.B906).

摘　　要：A series of 1-（1H-1,2,4-triazole-1-yl）-2-（2,4-difluoropheny1）-3-（N-isoproy1-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 7e exhibited more potent antifungal activities against nearly all fungi tested except AspergiUus fumigatus than fluconazole. ？2009 Qiu Ye Wu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All fights reserved.A series of 1-（1H-1,2,4-triazole-1-yl）-2-（2,4-difluoropheny1）-3-（N-isoproy1-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 7e exhibited more potent antifungal activities against nearly all fungi tested except AspergiUus fumigatus than fluconazole. ？2009 Qiu Ye Wu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All fights reserved.

关 键 词：TRIAZOLE SYNTHESIS Antifungal activity 

分 类 号：TQ426.8[化学工程] Q55[生物学—生物化学]