title: Aryl piperazine melanocortin MC4 receptor agonists.
abstract: Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.
authors.forename: Brian
authors.initials: B
authors.lastname: Dyck
authors.forename: Jessica
authors.initials: J
authors.lastname: Parker
authors.forename: Teresa
authors.initials: T
authors.lastname: Phillips
authors.forename: Lee
authors.initials: L
authors.lastname: Carter
authors.forename: Brian
authors.initials: B
authors.lastname: Murphy
authors.forename: Robin
authors.initials: R
authors.lastname: Summers
authors.forename: Julia
authors.initials: J
authors.lastname: Hermann
authors.forename: Tracy
authors.initials: T
authors.lastname: Baker
authors.forename: Mary
authors.initials: M
authors.lastname: Cismowski
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Val
authors.initials: V
authors.lastname: Goodfellow
mesh_terms: D002460:Cell Line; D000242:Cyclic AMP / Q000378:metabolism / Q000502:physiology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D007202:Indicators and Reagents; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4; D000242:Cyclic AMP