88857-57-2Relevant academic research and scientific papers
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R)
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.
, p. 3721 - 3725 (2007/10/03)
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.
