title: 4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
abstract: Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
authors.forename: Jinlong
authors.initials: J
authors.lastname: Jiang
authors.forename: Peter
authors.initials: P
authors.lastname: Lin
authors.forename: Myle
authors.initials: M
authors.lastname: Hoang
authors.forename: Lehua
authors.initials: L
authors.lastname: Chang
authors.forename: Carina
authors.initials: C
authors.lastname: Tan
authors.forename: Scott
authors.initials: S
authors.lastname: Feighner
authors.forename: Oksana C
authors.initials: OC
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: Nancy R
authors.initials: NR
authors.lastname: Morin
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: MacNeil
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Howard
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: D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001667:Binding, Competitive; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D066298:In Vitro Techniques; D015394:Molecular Structure; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin; C001920:4-aminoquinoline