title: Quinazoline and benzimidazole MCH-1R antagonists.
abstract: We have modified the previously reported 2-aminoquinoline 1 to provide two novel series of MCH-1R antagonists. Representative compounds from the quinazoline and benzimidazole series have been shown to be potent and selective, with promising in vitro eADME profiles.
authors.affiliation: Argenta Discovery Limited, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, UK.
authors.forename: Rosa
authors.initials: R
authors.lastname: Arienzo
authors.forename: Sue
authors.initials: S
authors.lastname: Cramp
authors.forename: Hazel J
authors.initials: HJ
authors.lastname: Dyke
authors.forename: Peter M
authors.initials: PM
authors.lastname: Lockey
authors.forename: Dennis
authors.initials: D
authors.lastname: Norman
authors.forename: Alan G
authors.initials: AG
authors.lastname: Roach
authors.forename: Phil
authors.initials: P
authors.lastname: Smith
authors.forename: Melanie
authors.initials: M
authors.lastname: Wong
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Wren
mesh_terms: D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011485:Protein Binding; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; C103263:MCHR1 protein, human; D011799:Quinazolines; D017481:Receptors, Somatostatin; C031000:benzimidazole