685126-24-3Relevant 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 (2004)
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.
Melanocortin-4 receptor binding compounds and methods of use thereof
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Page 103-107, (2008/06/13)
Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are a
