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ID: ALA1148424

Journal: Bioorg Med Chem Lett

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

Authors: Xi N, Hale C, Kelly MG, Norman MH, Stec M, Xu S, Baumgartner JW, Fotsch C.

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.

CiteXplore: 14698163

DOI: 10.1016/j.bmcl.2003.10.056