From lead to preclinical candidate: Optimization of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV

Sonja Nordhoff,Meritxell López-Canet,Barbara Hoffmann-Enger,Stephan Bulat,Silvia Cerezo-Gálvez,Oliver Hill,Claudia Rosenbaum,Christian Rummey,Meinolf Thiemann,Victor G. Matassa,Paul J. Edwards,Achim Feurer

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile.

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关键词

Dipeptidyl peptidase IV,DPP-4,DPP-IV,Type 2 diabetes,Glucagon-like peptide 1,GLP-1

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