| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372827 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The discovery and structure–activity relationship of 1,2-diarylimidazole piperazine carboxamides bearing polar side chains as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are described. Optimization of this series resulted in the discovery of isopropyl carboxamide 40, a CCK1R agonist with sub-nanomolar functional and binding activity as well as excellent potency in a mouse overnight food intake reduction assay.
Graphical abstractThe synthesis and biological profile of imidazole carboxamides of general structure 6 as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Richard Berger, Cheng Zhu, Alexa R. Hansen, Bart Harper, Zhesheng Chen, Tom G. Holt, James Hubert, Susan J. Lee, Jie Pan, Su Qian, Marc L. Reitman, Alison M. Strack, Drew T. Weingarth, Michael Wolff, Douglas J. MacNeil, Ann E. Weber, Scott D. Edmondson,