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.
引用
收藏
页码：4770 / 4773
页数：4
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