Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV
Journal of Medicinal Chemistry2010Vol. 54(2), pp. 510–524
Citations Over TimeTop 12% of 2010 papers
Zhiyuan Zhang, Michael B. Wallace, Jun Feng, Jeffrey A. Stafford, R.J. Skene, Lihong Shi, Bumsup Lee, Kathleen Aertgeerts, Andy Jennings, Rongda Xu, Daniel B. Kassel, Stephen W. Kaldor, Marc Navre, David R. Webb, Stephen L. Gwaltney
Abstract
The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.
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