The design of potent and selective inhibitors of DPP-4: Optimization of ADME properties by amide replacements

被引：21

作者：

Nordhoff, Sonja ^{[1
]}

Bulat, Stephan ^{[1
]}

Cerezo-Galvez, Silvia ^{[1
]}

Hill, Oliver ^{[1
]}

Hoffmann-Enger, Barbara ^{[1
]}

Lopez-Canet, Meritxell ^{[1
]}

Rosenbaum, Claudia ^{[1
]}

Rummey, Christian ^{[1
]}

Thiemann, Meinolf ^{[1
]}

Matassa, Victor G. ^{[1
]}

Edwards, Paul J. ^{[1
]}

Feurer, Achim ^{[1
]}

机构：

[1] Santhera Pharmaceut Switzerland Ltd, CH-4410 Liestal, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 22期

关键词：

Dipeptidyl peptidase IV; DPP-IV; DPP-4; Type; 2; diabetes; Glucagon-like peptide 1; GLP-1; DIPEPTIDYL-PEPTIDASE-IV; GLUCAGON-LIKE PEPTIDE-1; HIGHLY POTENT; DISCOVERY; ALKYNES; AZIDES;

D O I：

10.1016/j.bmcl.2009.09.078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

For a series of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV ADME properties were improved by the incorporation of amide replacements. These efforts led to a novel series of potent and selective inhibitors of DPP-4 that exhibit an attractive pharmacokinetic profile and show excellent efficacy in an animal model of diabetes. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6340 / 6345

页数：6

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