Design,synthesis and antifungal activities in vitro of novel tetralin compounds
Design,synthesis and antifungal activities in vitro of novel tetralin compounds作者机构：Department of Medicinal Chemistry School of Pharmacy Second Military Medical University Shanghai 200433 China
出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)
年 卷 期：2008年第19卷第3期
页 面：264-268页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 0703[理学-化学] 10[医学]
基 金：National Natural Science Foundation of China NSFC: 30572257
主 题：Antifungal Chiral tetralins Lanosterol 14α-demethylase Design Synthesis
摘 要：Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of Candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhihitars of fungi.
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