Design, Synthesis and Biological Evaluation of Non-azole Inhibitors of Lanosterol 14α-Demethylase of Fungi  

作　　者：Bin YAO You Jun ZHOU Jü ZHU Jia Guo Lü Yao Wu LI Jun CHENG Qing Feng JIANG Can Hui ZHENG 

机构地区：[1]School of Pharmacy, Second Military Medicial University, Shanghai 200433

出　　处：《Chinese Chemical Letters》2006年第9期1189-1192,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.30572257)

摘　　要：Novel tetralin compounds were designed and synthesized on the three-dimensional model of lanosterol 14α-demethylase of Candida albicans. All of the lead compounds exhibited potent antifungal activities, especially compounds 16, 20. The mode of the action of the lead compounds was different from that of azoles. The present study affords the possibility to develop novel antifungal agents that specifically interact with the amino acid residues in the active site and avoid the serious toxicity arising from coordination binding with the heme of mammalian P450s.

关 键 词：ANTIFUNGAL 2-aminotetralins lanosterol 14α-demethylase inhibitor. 

分 类 号：R978.5[医药卫生—药品] R914.4[医药卫生—药学]