| Literature DB >> 17441705 |
Jun Feng, Zhiyuan Zhang, Michael B Wallace, Jeffrey A Stafford, Stephen W Kaldor, Daniel B Kassel, Marc Navre, Lihong Shi, Robert J Skene, Tomoko Asakawa, Koji Takeuchi, Rongda Xu, David R Webb, Stephen L Gwaltney.
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.Entities:
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Year: 2007 PMID： 17441705 DOI： 10.1021/jm070104l
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446