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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.

Abstract：

:Dipeptidyl peptidase IV (DPP4) is a multifunctional type II transmembrane serine peptidase which regulates various physiological processes, most notably plasma glucose homeostasis by cleaving peptide hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. Inhibition of DPP4 is a potentially valuable therapy for type 2 diabetes. Synthesis and structure-activity relationships of a series of substituted diprolyl nitriles are described, leading to the identification of compound 1 with a measured DPP4 K(i) of 3.6 nM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhao G,Taunk PC,Magnin DR,Simpkins LM,Robl JA,Wang A,Robertson JG,Marcinkeviciene J,Sitkoff DF,Parker RA,Kirby MS,Hamann LG

doi

10.1016/j.bmcl.2005.06.043

subject

Has Abstract

pub_date

2005-09-15 00:00:00

pages

3992-5

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00794-8

journal_volume

15

pub_type

杂志文章

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