Hit-to-lead optimization of pyrrolo[1,2-a]quinoxalines as novel cannabinoid type 1 receptor antagonists.
Hit-to-lead optimization of a novel series of N-alkyl-N-[2-oxo-2-(4-aryl-4H-pyrrolo[1,2-a]quinoxaline-5-yl)-ethyl]-carboxylic acid amides, derived from a high throughput screening (HTS) hit, are described. Subsequent optimization led to identification of in vitro potent cannabinoid 1 receptor (CB1R) antagonists representing a new class of compounds in this area.
Szabó
György
G
Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary. gy.szabo@richter.hu
Kiss
Róbert
R
Páyer-Lengyel
Dóra
D
Vukics
Krisztina
K
Szikra
Judit
J
Baki
Andrea
A
Molnár
László
L
Fischer
János
J
Keseru
György M
GM
D000818:Animals; D001665:Binding Sites; D003198:Computer Simulation; D010880:Piperidines / Q000737:chemistry; D011720:Pyrazoles / Q000737:chemistry; D011810:Quinoxalines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000077285:Rimonabant; D013329:Structure-Activity Relationship
D010880:Piperidines; D011720:Pyrazoles; D011810:Quinoxalines; D043884:Receptor, Cannabinoid, CB1; D000077285:Rimonabant