title: The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.
abstract: The design, synthesis, and biological studies of a novel class of MCH-R1 antagonists based on an aminotetrahydronaphthalene ketopiperazine scaffold is described. Compounds within this class promoted significant body weight reduction in mouse diet induced obesity studies. The potential for hERG blockage activity and QT interval studies in anesthetized dogs are discussed.
authors.affiliation: Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA. mendezandino.jl@pg.com
authors.forename: José L
authors.initials: JL
authors.lastname: Méndez-Andino
authors.forename: Anny-Odile
authors.initials: AO
authors.lastname: Colson
authors.forename: Kenneth M
authors.initials: KM
authors.lastname: Meyers
authors.forename: Maria C
authors.initials: MC
authors.lastname: Mitchell
authors.forename: Karen
authors.initials: K
authors.lastname: Hodge
authors.forename: Jeremy M
authors.initials: JM
authors.lastname: Howard
authors.forename: Nicholas
authors.initials: N
authors.lastname: Kim
authors.forename: David C
authors.initials: DC
authors.lastname: Ackley
authors.forename: Jerry K
authors.initials: JK
authors.lastname: Holbert
authors.forename: Scott W
authors.initials: SW
authors.lastname: Mittelstadt
authors.forename: Martin E
authors.initials: ME
authors.lastname: Dowty
authors.forename: Cindy M
authors.initials: CM
authors.lastname: Obringer
authors.forename: Paula
authors.initials: P
authors.lastname: Suchanek
authors.forename: Ofer
authors.initials: O
authors.lastname: Reizes
authors.forename: X Eric
authors.initials: XE
authors.lastname: Hu
authors.forename: John A
authors.initials: JA
authors.lastname: Wos
mesh_terms: D000818:Animals; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: C103263:MCHR1 protein, human; D010879:Piperazines; D017481:Receptors, Somatostatin