Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors

被引：19

作者：

Kurukulasuriya, Ravi ^{[1
]}

Rohde, Jeffrey J. ^{[1
]}

Szczepankiewicz, Bruce G. ^{[1
]}

Basha, Fatima ^{[1
]}

Lai, Chunqui ^{[1
]}

Jae, Hwan-Soo ^{[1
]}

Winn, Martin ^{[1
]}

Stewart, Kent D. ^{[1
]}

Longenecker, Kenton L. ^{[1
]}

Lubben, Thomas W. ^{[1
]}

Ballaron, Stephen J. ^{[1
]}

Sham, Hing L. ^{[1
]}

von Geldern, Thomas W. ^{[1
]}

机构：

[1] Abbott Labs, Metabol Dis Res, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 24期

关键词：

dipeptidyl peptidase IV (DPPIV); xanthines; SAR; X-ray structure; type; 2; diabetes;

D O I：

10.1016/j.bmcl.2006.09.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K-i = 2 nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6226 / 6230

页数：5

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