title: Structure-activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor.
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.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Tran
authors.forename: Joseph
authors.initials: J
authors.lastname: Pontillo
authors.forename: Melissa
authors.initials: M
authors.lastname: Arellano
authors.forename: Beth A
authors.initials: BA
authors.lastname: Fleck
authors.forename: Fabio C
authors.initials: FC
authors.lastname: Tucci
authors.forename: Dragan
authors.initials: D
authors.lastname: Marinkovic
authors.forename: Caroline W
authors.initials: CW
authors.lastname: Chen
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: D000577:Amides / Q000737:chemistry*; D001667:Binding, Competitive; D006801:Humans; D008968:Molecular Conformation; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D044104:Receptor, Melanocortin, Type 3 / Q000037:antagonists & inhibitors; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; C470072:MC4R protein, human; D010880:Piperidines; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4