Quinazoline and benzimidazole MCH-1R antagonists.
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.
Arienzo
Rosa
R
Argenta Discovery Limited, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, UK.
Cramp
Sue
S
Dyke
Hazel J
HJ
Lockey
Peter M
PM
Norman
Dennis
D
Roach
Alan G
AG
Smith
Phil
P
Wong
Melanie
M
Wren
Stephen P
SP
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
D001562:Benzimidazoles; C103263:MCHR1 protein, human; D011799:Quinazolines; D017481:Receptors, Somatostatin; C031000:benzimidazole