Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371982 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A new series of CB1 receptor antagonists incorporating an imidazole-based isosteric replacement for the hydrazide moiety of rimonabant (SR141716) is disclosed. Members of this imidazole series possess potent/selective binding to the rCB1 receptor and exhibit potent hCB1 functional activity. Isopropyl analog 9a demonstrated activity in the tetrad assay and was orally-active in a food intake model.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert L. Dow, John R. Hadcock, Dennis O. Scott, Steven R. Schneider, Ernest S. Paight, Philip A. Iredale, Philip A. Carpino, David A. Griffith, Marlys Hammond, Paul DaSilva-Jardine,