| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373129 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The design and synthesis of a GPR119 agonist bearing a 2-(2,3,6-trifluorophenyl)acetamide group is described. The design capitalized on the conformational restriction found in N-β-fluoroethylamide derivatives to help maintain good levels of potency while driving down both lipophilicity and oxidative metabolism in human liver microsomes. The chemical stability and bioactivation potential are discussed.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Vincent Mascitti, Benjamin D. Stevens, Chulho Choi, Kim F. McClure, Cristiano R.W. Guimarães, Kathleen A. Farley, Michael J. Munchhof, Ralph P. Robinson, Kentaro Futatsugi, Sophie Y. Lavergne, Bruce A. Lefker, Peter Cornelius, Paul D. Bonin,