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J Med Chem. 2007 May 17;50(10):2297-300. Epub 2007 Apr 19.

Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.

Erratum in

  • J Med Chem. 2008 Jul 24;51(14):4357.

Abstract

Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4). Herein, we describe the structure-based design and optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors. Following an oral dose, these noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and a lowering of blood glucose in animal models of diabetes. Alogliptin is currently undergoing phase III trials in patients with type 2 diabetes.

PMID:
17441705
DOI:
10.1021/jm070104l
[Indexed for MEDLINE]
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