An aminomethylpyrimidine DPP-IV inhibitor with improved properties

被引：41

作者：

Peters, JU ^{[1
]}

Hunziker, D ^{[1
]}

Fischer, H ^{[1
]}

Kansy, M ^{[1
]}

Weber, S ^{[1
]}

Kritter, S ^{[1
]}

Müller, A ^{[1
]}

Wallier, A ^{[1
]}

Ricklin, F ^{[1
]}

Boehringer, M ^{[1
]}

Poli, SM ^{[1
]}

Csato, M ^{[1
]}

Loeffler, BM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 13期

关键词：

D O I：

10.1016/j.bmcl.2004.04.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A recently identified DPP-IV inhibitor (1) was found to induce phospholipidosis and to inhibit CYP3A4. A small series of less lipophilic and less amphiphilic analogues was synthesized in an effort to overcome these issues. One compound from this series was equipotent to 1, did not induce phospholipidosis and showed a reduced CYP3A4 inhibition. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3575 / 3578

页数：4

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