| Literature DB >> 15203150 |
Thomas H Marsilje1, Jonathan B Roses, Emily F Calderwood, Stephen G Stroud, Nancy E Forsyth, Christopher Blackburn, David L Yowe, Wenyan Miao, Stacey V Drabic, Marie D Bohane, J Scott Daniels, Ping Li, Lijun Wu, Michael A Patane, Christopher F Claiborne.
Abstract
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.Entities:
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Year: 2004 PMID： 15203150 DOI： 10.1016/j.bmcl.2004.05.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823