title: Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
abstract: A series of 2-pyridinylpiperazines derived from beta-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki=6.5 nM) possessed high potency.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors.forename: Joe A
authors.initials: JA
authors.lastname: Tran
authors.forename: Joseph
authors.initials: J
authors.lastname: Pontillo
authors.forename: Beth A
authors.initials: BA
authors.lastname: Fleck
authors.forename: Dragan
authors.initials: D
authors.lastname: Marinkovic
authors.forename: Melissa
authors.initials: M
authors.lastname: Arellano
authors.forename: Fabio C
authors.initials: FC
authors.lastname: Tucci
authors.forename: Marion
authors.initials: M
authors.lastname: Lanier
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Wanlong
authors.initials: W
authors.lastname: Jiang
authors.forename: Caroline W
authors.initials: CW
authors.lastname: Chen
authors.forename: Alan C
authors.initials: AC
authors.lastname: Foster
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D004151:Dipeptides / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D015091:beta-Alanine / Q000737:chemistry
chemical_list: D004151:Dipeptides; D010879:Piperazines; D011725:Pyridines; D044105:Receptor, Melanocortin, Type 4; D015091:beta-Alanine