title: Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
abstract: The synthesis and biological testing of novel classes of potent melanin-concentrating hormone (MCH-R1) antagonists based on pyrazolopiperazinone and pyrrolopiperazinone scaffolds are described.
authors.affiliation: Procter and Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.
authors.forename: Kenneth M
authors.initials: KM
authors.lastname: Meyers
authors.forename: José
authors.initials: J
authors.lastname: Méndez-Andino
authors.forename: Anny-Odile
authors.initials: AO
authors.lastname: Colson
authors.forename: X Eric
authors.initials: XE
authors.lastname: Hu
authors.forename: John A
authors.initials: JA
authors.lastname: Wos
authors.forename: Maria C
authors.initials: MC
authors.lastname: Mitchell
authors.forename: Karen
authors.initials: K
authors.lastname: Hodge
authors.forename: Jeremy
authors.initials: J
authors.lastname: Howard
authors.forename: Jennifer L
authors.initials: JL
authors.lastname: Paris
authors.forename: Martin E
authors.initials: ME
authors.lastname: Dowty
authors.forename: Cindy M
authors.initials: CM
authors.lastname: Obringer
authors.forename: Ofer
authors.initials: O
authors.lastname: Reizes
mesh_terms: D018938:Caco-2 Cells; D006801:Humans; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D044405:Receptor, Serotonin, 5-HT2C / Q000187:drug effects; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*
chemical_list: D007202:Indicators and Reagents; C103263:MCHR1 protein, human; D010879:Piperazines; D011720:Pyrazoles; D011758:Pyrroles; D044405:Receptor, Serotonin, 5-HT2C; D017481:Receptors, Somatostatin; C518524:pyrazolopiperazinone; C518525:pyrrolopiperazinone