New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors

被引：35

作者：

Hulin, B ^{[1
]}

Cabral, S ^{[1
]}

Lopaze, MG ^{[1
]}

Van Volkenburg, MA ^{[1
]}

Andrews, KM ^{[1
]}

Parker, JC ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期

关键词：

dipeptidyl peptidase IV; DPP-IV; cyclohexylglycine; difluoropyrrolidine; tetrafluoropyrrolidine; fluoroazetidine; difluoroazetidine;

D O I：

10.1016/j.bmcl.2005.07.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cyclohexylglycine amides of various fluorinated pyrrolidines and azetidines were prepared and tested for activity against dipeptidyl peptidase IV and in vivo in the KK mouse model of type 2 diabetes. The tetrafluoropyrrolidide, cis-3,4-difluoropyrrolidide and the fluorinated azetidides displayed unexpectedly strong activity. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：4770 / 4773

页数：4

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