title: 6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts.
abstract: SAR explorations of the eastern and western parts of recently disclosed 2-aminoquinoline MCH1R-antagonists are reported. Eastern part investigations confirmed a high degree of structural freedom, and a number of additional single digit nanomolar antagonists were identified. Investigations of the western part also confirmed the initial SAR analysis, requiring a para-substituted phenyl ring spaced from the 6-amide by two connecting atoms. The exploration led to the discovery of a novel sub-series with a 4-biphenylcarboxamide western part, also exhibiting single digit nanomolar affinity.
authors.affiliation: 7TM Pharma A/S, Fremtidsvej 3, DK-2970 Hørsholm, Denmark.
authors.forename: Trond
authors.initials: T
authors.lastname: Ulven
authors.forename: Paul Brian
authors.initials: PB
authors.lastname: Little
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Receveur
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Frimurer
authors.forename: Oystein
authors.initials: O
authors.lastname: Rist
authors.forename: Pia K
authors.initials: PK
authors.lastname: Nørregaard
authors.forename: Thomas
authors.initials: T
authors.lastname: Högberg
mesh_terms: D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D011804:Quinolines; D017481:Receptors, Somatostatin