title: 2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
abstract: A series of 2-aminoquinoline compounds was prepared and evaluated in MCH1R binding and functional antagonist assays. Small dialkyl, methylalkyl, methylcycloalkyl, and cyclic amines were tolerated at the quinoline 2-position. The in vivo efficacy of compound 12 was explored and compared to that of a related inactive analog to determine their effects on food intake and body weight in rodents.
authors.affiliation: Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065-0900, USA.
authors.forename: Jinlong
authors.initials: J
authors.lastname: Jiang
authors.forename: Myle
authors.initials: M
authors.lastname: Hoang
authors.forename: Jonathan R
authors.initials: JR
authors.lastname: Young
authors.forename: Danny
authors.initials: D
authors.lastname: Chaung
authors.forename: Ronsar
authors.initials: R
authors.lastname: Eid
authors.forename: Cherilyn
authors.initials: C
authors.lastname: Turner
authors.forename: Peter
authors.initials: P
authors.lastname: Lin
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Junying
authors.initials: J
authors.lastname: Wang
authors.forename: Carina
authors.initials: C
authors.lastname: Tan
authors.forename: Scott
authors.initials: S
authors.lastname: Feighner
authors.forename: Oksana
authors.initials: O
authors.lastname: Palyha
authors.forename: Donna L
authors.initials: DL
authors.lastname: Hreniuk
authors.forename: Jie
authors.initials: J
authors.lastname: Pan
authors.forename: Andreas W
authors.initials: AW
authors.lastname: Sailer
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: MacNeil
authors.forename: Andrew
authors.initials: A
authors.lastname: Howard
authors.forename: Lauren
authors.initials: L
authors.lastname: Shearman
authors.forename: Sloan
authors.initials: S
authors.lastname: Stribling
authors.forename: Ramon
authors.initials: R
authors.lastname: Camacho
authors.forename: Alison
authors.initials: A
authors.lastname: Strack
authors.forename: Lex H T
authors.initials: LH
authors.lastname: Van der Ploeg
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
authors.forename: Robert J
authors.initials: RJ
authors.lastname: DeVita
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D004435:Eating; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011812:Quinuclidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: C515121:6-(12-(2-fluoromethylpyridin-5-yl)dodecanamido)-2-(1-quinuclidinyl)quinoline; C103263:MCHR1 protein, human; C491208:MCHR1 protein, rat; D011804:Quinolines; D011812:Quinuclidines; D017481:Receptors, Somatostatin