Article ID Journal Published Year Pages File Type
1377598 Bioorganic & Medicinal Chemistry Letters 2007 5 Pages PDF
Abstract

A series of β-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the β-aminoamide series, which ultimately led to the discovery of JANUVIA™ (sitagliptin phosphate, compound 1), are described.

Graphical abstractA series of β-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , , , , , , , , , ,