Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents

被引：139

作者：

Ahn, JH ^{[1
]}

Kim, HM ^{[1
]}

Jung, SH ^{[1
]}

Kang, SK ^{[1
]}

Kim, KR ^{[1
]}

Rhee, SD ^{[1
]}

Yang, SD ^{[1
]}

Cheon, HG ^{[1
]}

Kim, SS ^{[1
]}

机构：

[1] Korea Res Inst Chem Technol, Div Med Sci, Taejon 305600, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 17期

关键词：

dipeptidyl peptidase IV; DP-IV; pyrazoline; anti-diabetic agent;

D O I：

10.1016/j.bmcl.2004.06.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of cyano-pyrazoline derivatives with a secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4461 / 4465

页数：5

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