Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors

被引：38
|
作者：
Ahn, JH [1 ]
Kim, JA
Kim, HM
Kwon, HM
Huh, SC
Rhee, SD
Kim, KR
Yang, SD
Park, SD
Lee, JM
Kim, SS
Cheon, HG
机构：
[1] Korea Res Inst Chem Technol, Div Med Sci, Taejon 305600, South Korea
[2] JEIL Pharmaceut Co Ltd, R&D Ctr, Yongin 449861, South Korea
[3] CJ Corp, R&D Ctr Pharmaceut, Ichon 467810, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期
关键词：
dipeptidyl peptidase IV; DP-IV; pyrazolidine; anti-diabetic agent;
D O I：
10.1016/j.bmcl.2005.01.020
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56 mu M and ED50 value of 80 mg/kg (in vivo DP-IV inhibition; po). (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1337 / 1340
页数：4
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