title: Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
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%).
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors.forename: Joseph
authors.initials: J
authors.lastname: Pontillo
authors.forename: Joe A
authors.initials: JA
authors.lastname: Tran
authors.forename: Nicole S
authors.initials: NS
authors.lastname: White
authors.forename: Melissa
authors.initials: M
authors.lastname: Arellano
authors.forename: Beth A
authors.initials: BA
authors.lastname: Fleck
authors.forename: Dragan
authors.initials: D
authors.lastname: Marinkovic
authors.forename: Fabio C
authors.initials: FC
authors.lastname: Tucci
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Alan C
authors.initials: AC
authors.lastname: Foster
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D044482:Benzeneacetamides / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D044482:Benzeneacetamides; D008024:Ligands; C470072:MC4R protein, human; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4