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
收藏
页码：3268 / 3272
页数：5
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