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Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

Bioorganic & medicinal chemistry letters (2003-12-31)
Ning Xi, Clarence Hale, Michael G Kelly, Mark H Norman, Markian Stec, Shimin Xu, James W Baumgartner, Christopher Fotsch
ABSTRACT

A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC(50)s ranging from <0.1 to 200 nM). Both agonists and antagonists of MC4R were prepared by modifying the groups attached to the right-hand side of the succinamide. This series also exhibits a high level of selectivity (up to 7000-fold) over mouse MC1R and human MC3R.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
(Bromomethyl)cyclopropane, 97%
Sigma-Aldrich
Succinamide, 98%

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