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

页码：1337 / 1340

页数：4

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