title: Hit-to-lead optimization of pyrrolo[1,2-a]quinoxalines as novel cannabinoid type 1 receptor antagonists.
abstract: 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.
authors.affiliation: Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary. gy.szabo@richter.hu
authors.forename: György
authors.initials: G
authors.lastname: Szabó
authors.forename: Róbert
authors.initials: R
authors.lastname: Kiss
authors.forename: Dóra
authors.initials: D
authors.lastname: Páyer-Lengyel
authors.forename: Krisztina
authors.initials: K
authors.lastname: Vukics
authors.forename: Judit
authors.initials: J
authors.lastname: Szikra
authors.forename: Andrea
authors.initials: A
authors.lastname: Baki
authors.forename: László
authors.initials: L
authors.lastname: Molnár
authors.forename: János
authors.initials: J
authors.lastname: Fischer
authors.forename: György M
authors.initials: GM
authors.lastname: Keseru
mesh_terms: 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
chemical_list: D010880:Piperidines; D011720:Pyrazoles; D011810:Quinoxalines; D043884:Receptor, Cannabinoid, CB1; D000077285:Rimonabant