期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 10, 页码 2297-2300出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm070104l
关键词
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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.
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