Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARγ ligands (I)

被引：12

作者：

Dong, Xiaochun

Zhang, Zhenshan

Wen, Ren ^{[1
]}

Shen, Jianhua

Shen, Xu

Jiang, Hualiang

机构：

[1] Fudan Univ, Dept Med Chem, Shanghai 200032, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 22期

关键词：

de novo drug design; PPAR gamma ligand; type II diabetes; indole compounds;

D O I：

10.1016/j.bmcl.2006.06.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

MCSS and LeapFrog, two de novo drug design programs, were used for the novel indole-based PPAR gamma ligands' study. The designed compounds were synthesized and tested for the PPAR gamma protein binding activities in vitro. Out of the compounds that were synthesized, two molecules (compounds 14d and 7d) possessed potent PPAR gamma protein binding activity close to rosiglitazone in vitro. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：5913 / 5916

页数：4

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