title: Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
abstract: A new series of 2-aminoquinolines has been identified as antagonists of the melanin concentrating hormone receptor (MCH-1R). Syntheses and structure-activity relationships are described leading to a compound having low nanomolar activity against the receptor and demonstrating functional antagonism. Studies also showed that some of the compounds were selective against a range of other G protein-coupled receptors.
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: David E
authors.initials: DE
authors.lastname: Clark
authors.forename: Sue
authors.initials: S
authors.lastname: Cramp
authors.forename: Stephen
authors.initials: S
authors.lastname: Daly
authors.forename: Hazel J
authors.initials: HJ
authors.lastname: Dyke
authors.forename: Peter
authors.initials: P
authors.lastname: Lockey
authors.forename: Dennis
authors.initials: D
authors.lastname: Norman
authors.forename: Alan G
authors.initials: AG
authors.lastname: Roach
authors.forename: Keith
authors.initials: K
authors.lastname: Stuttle
authors.forename: Maxine
authors.initials: M
authors.lastname: Tomlinson
authors.forename: Melanie
authors.initials: M
authors.lastname: Wong
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Wren
mesh_terms: D006801:Humans; D007700:Kinetics; D008968:Molecular Conformation; D010879:Piperazines / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D010880:Piperidines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor