Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor

Joseph Pontillo; Joe A Tran; Nicole S White; Melissa Arellano; Beth A Fleck; Dragan Marinkovic; Fabio C Tucci; John Saunders; Alan C Foster; Chen Chen

doi:10.1016/j.bmcl.2005.08.061

Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5237-40. doi: 10.1016/j.bmcl.2005.08.061. Epub 2005 Sep 23.

Authors

Joseph Pontillo¹, Joe A Tran, Nicole S White, Melissa Arellano, Beth A Fleck, Dragan Marinkovic, Fabio C Tucci, John Saunders, Alan C Foster, Chen Chen

Affiliation

¹ Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA.

PMID: 16183282
DOI: 10.1016/j.bmcl.2005.08.061

Abstract

Synthesis and structure-activity relationship studies of a series of cyclohexylpiperazines bearing an amide side chain as ligands of the MC4 receptor are discussed. Compounds such as 11i from this series are potent agonists (EC(50)=33nM, IA=96%).

MeSH terms

Benzeneacetamides / chemistry*
Humans
Ligands
Piperazines / chemical synthesis
Piperazines / chemistry*
Piperazines / pharmacology*
Receptor, Melanocortin, Type 4 / agonists*
Structure-Activity Relationship

Substances

Benzeneacetamides
Ligands
MC4R protein, human
Piperazines
Receptor, Melanocortin, Type 4