(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: A potent, selective, orally active dipeptidyl peptidase IV inhibitor

Mark J. Ammirati,Kim M. Andrews,David D. Boyer,Anne M. Brodeur,Dennis E. Danley,Shawn D. Doran,Bernard Hulin,Shenping Liu,R. Kirk McPherson,Stephen J. Orena,Janice C. Parker,Jana Polivkova,Xiayang Qiu,Carolyn B. Soglia,Judith L. Treadway,Maria A. VanVolkenburg,Donald C. Wilder,David W. Piotrowski

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

A series of 4-substituted proline amides was evaluated as inhibitors of dipeptidyl pepdidase IV for the treatment of type 2 diabetes. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone (5) emerged as a potent (IC50=13nM) and selective compound, with high oral bioavailability in preclinical species.

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关键词

Dipeptidyl peptidase IV,DPP-4,Diabetes

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