1.
Bioorg Med Chem Lett
; 14(14): 3721-5, 2004 Jul 16.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15203150
RESUMEN
A novel series of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R) is reported. Members of this series have been identified, which exhibit sub-micromolar binding affinity for the MC4-R, functional potency <100nM, and good oral exposure in rat. Antagonists of the MC4-R are potentially useful in the therapeutic treatment of involuntary weight loss due to advanced age or disease (e.g. cancer or AIDS), an area of large, unmet medical need.