Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors

被引：63

作者：

Caldwell, CG

Chen, P

He, JF

Parmee, ER

Leiting, B

Marsilio, F

Patel, RA

Wu, JK

Eiermann, GJ

Petrov, A

He, HB

Lyons, KA

Thornberry, NA

Weber, AE

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Metab Disorders Diabetes, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Anim Pharmacol, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Basic Chem, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 05期

关键词：

D O I：

10.1016/j.bmcl.2003.12.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：1265 / 1268

页数：4

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