Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
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.
Arienzo
Rosa
R
Argenta Discovery Limited, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, UK.
Clark
David E
DE
Cramp
Sue
S
Daly
Stephen
S
Dyke
Hazel J
HJ
Lockey
Peter
P
Norman
Dennis
D
Roach
Alan G
AG
Stuttle
Keith
K
Tomlinson
Maxine
M
Wong
Melanie
M
Wren
Stephen P
SP
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
D010879:Piperazines; D010880:Piperidines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor