Aminomethylpyrimidines as novel DPP-IV inhibitors:: A 105-fold activity increase by optimization of aromatic substituents

被引：73

作者：

Peters, JU ^{[1
]}

Weber, S ^{[1
]}

Kritter, S ^{[1
]}

Weiss, P ^{[1
]}

Wallier, A ^{[1
]}

Boehringer, M ^{[1
]}

Hennig, M ^{[1
]}

Kuhn, B ^{[1
]}

Loeffler, BM ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Preclin Res, Div Pharma, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2004.01.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1491 / 1493

页数：3

共 24 条

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