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

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.

journal_name

Bioorg Med Chem Lett

authors

Marsilje TH,Roses JB,Calderwood EF,Stroud SG,Forsyth NE,Blackburn C,Yowe DL,Miao W,Drabic SV,Bohane MD,Daniels JS,Li P,Wu L,Patane MA,Claiborne CF

doi

10.1016/j.bmcl.2004.05.003

subject

Has Abstract

pub_date

2004-07-16 00:00:00

pages

3721-5

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960894X04006225

journal_volume

14

pub_type

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