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Bioorg Med Chem Lett. 2004 Jul 16;14(14):3721-5.

Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).

Author information

1
Department of Medicinal Chemistry, Millennium Pharmaceuticals, Inc., Cambridge, MA 02139, USA. tmarsiljie@gnf.org

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.

PMID:
15203150
DOI:
10.1016/j.bmcl.2004.05.003
[Indexed for MEDLINE]

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