Design, synthesis and antifungal activities in vitro of novel tetralin compounds

被引：7

作者：

Hui Tang ^{[1
]}

You Jun Zhou ^{[1
]}

Yao Wu Li ^{[1
]}

Jia Guo Lv ^{[1
]}

Can Hui Zheng ^{[1
]}

Jun Chen ^{[1
]}

Ju Zhu ^{[1
]}

机构：

[1] Mil Med Univ 2, Sch Pharm, Dept Med Chem, Shanghai 200433, Peoples R China

来源：

CHINESE CHEMICAL LETTERS | 2008年 / 19卷 / 03期

基金：

中国国家自然科学基金;

关键词：

antifungal; chiral tetralins; lanosterol; 14; alpha-demethylase; design; synthesis;

D O I：

10.1016/j.cclet.2007.12.031

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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 inhibitors of fungi. (c) 2007 Ju Zhu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

引用

页码：264 / 268

页数：5

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