Structure Report for: 3G0B

Zhang, Zhiyuan, Wallace, Michael B., Feng, Jun, Stafford, Jeffrey A., Kaldor, Stephen W., Lihong, Shi, Skene, Robert J., Aertgeerts, Kathleen, Lee, Bumsup, Jennings, Andy, Xu, Rongda, Kassel, Daniel, Webb, David R., Gwaltney, Stephen L.

Title: Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A and Gwaltney SL <5 more author(s)> Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL (- 5)
Ref: Journal of Medicinal Chemistry, 54:510, 2011 : PubMed
Abstract


ESTHER: Zhang_2011_J.Med.Chem_54_510
PubMedSearch: Zhang 2011 J.Med.Chem 54 510
PubMedID: 21186796
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Pyrimidinone-inhibitor1, Pyrimidinone-inhibitor3, Xanthine-inhibitor-4, CHEMBL2159182, Alogliptin

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.