Bioorganic and Medicinal Chemistry Letters p. 3721 - 3725 (2004)
Update date:2022-08-04
Topics:
Marsilje, Thomas H.
Roses, Jonathan B.
Calderwood, Emily F.
Stroud, Stephen G.
Forsyth, Nancy E.
Blackburn, Christopher
Yowe, David L.
Miao, Wenyan
Drabic, Stacey V.
Bohane, Marie D.
Daniels, J. Scott
Li, Ping
Wu, Lijun
Patane, Michael A.
Claiborne, Christopher F.
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.
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