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Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: Potent, orally-active 1,4-disubstituted imidazoles |
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| 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 |
| Affiliation: | aPfizer Global Research and Development, Groton, CT 06340, USA |
| 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. |
| Keywords: | Cannabinoid-1 receptor antagonist SR-141716 Imidazole isostere Food intake inhibition |
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