Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors

被引：16

作者：

Tsai, Ting-Yueh ^{[1
]}

Coumar, Mohane Selvaraj ^{[1
]}

Hsu, Tsu ^{[1
]}

Hsieh, Hsing-Pang ^{[1
]}

Chien, Chia-Hui ^{[1
]}

Chen, Chiung-Tong ^{[1
]}

Chang, Chung-Nien ^{[1
]}

Lo, Yu-Kang ^{[1
]}

Wu, Ssu-Hui ^{[1
]}

Huang, Chung-Yu ^{[1
]}

Huang, Yu-Wen ^{[1
]}

Wang, Min-Hsien ^{[1
]}

Wu, Hsin-Yi ^{[1
]}

Lee, Hong-Jen ^{[1
]}

Chen, Xin ^{[1
]}

Chao, Yu-Sheng ^{[1
]}

Jiaang, Weir-Torn ^{[1
]}

机构：

[1] Natl Hlth Res Inst, Div Biotechnol & Pharmaceut Res, Miaoli 350, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 12期

关键词：

DPP-IV; diabetes; pyrrolidine;

D O I：

10.1016/j.bmcl.2006.03.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3268 / 3272

页数：5

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