Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor

Joseph A Tran; Joseph Pontillo; Melissa Arellano; Beth A Fleck; Fabio C Tucci; Dragan Marinkovic; Caroline W Chen; John Saunders; Alan C Foster; Chen Chen

doi:10.1016/j.bmcl.2005.05.017

Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3434-8. doi: 10.1016/j.bmcl.2005.05.017.

Authors

Joseph A Tran¹, Joseph Pontillo, Melissa Arellano, Beth A Fleck, Fabio C Tucci, Dragan Marinkovic, Caroline W Chen, 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: 15950470
DOI: 10.1016/j.bmcl.2005.05.017

Abstract

A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity (Ki) of 4.2 and 1100 nM at MC4R and MC3R, respectively.

MeSH terms

Amides / chemistry*
Binding, Competitive
Humans
Molecular Conformation
Piperidines / chemical synthesis
Piperidines / chemistry
Piperidines / pharmacology*
Receptor, Melanocortin, Type 3 / antagonists & inhibitors
Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Amides
MC4R protein, human
Piperidines
Receptor, Melanocortin, Type 3
Receptor, Melanocortin, Type 4