| Autor: |
Palani, A., Shapiro, S., McBriar, M. D., Clader, J. W., Greenlee, W. J., Spar, B., Kowalski, T. J., Farley, C., Cook, J., Heek, M. van, Weig, B., O'Neill, K., Graziano, M., Hawes, B. |
| Zdroj: |
Journal of Medicinal Chemistry; July 2005, Vol. 48 Issue: 15 p4746-4749, 4p |
| Abstrakt: |
Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure−activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound 1 exhibited oral efficacy in chronic (28 d) rodent models at 3−30 mpk showing significant reduction in food intake and weight gain relative to controls. |
| Databáze: |
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