title: Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles.
abstract: A variety of pyrido[1,2-a]benzimidazoles (PBIs) modified on the A-ring were prepared and evaluated for affinity to the benzodiazepine binding site on the GABA-A receptor and in animal models predictive of anxiolytic activity in humans. A-ring benzo-fused derivative 7 exhibited potent activity, as did the 6- and 7-pyrido compounds 3 and 4.
authors.affiliation: Drug Discovery, R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA.
authors.forename: B E
authors.initials: BE
authors.lastname: Maryanoff
authors.forename: S O
authors.initials: SO
authors.lastname: Nortey
authors.forename: J J
authors.initials: JJ
authors.lastname: McNally
authors.forename: P J
authors.initials: PJ
authors.lastname: Sanfilippo
authors.forename: D F
authors.initials: DF
authors.lastname: McComsey
authors.forename: B
authors.initials: B
authors.lastname: Dubinsky
authors.forename: R P
authors.initials: RP
authors.lastname: Shank
authors.forename: A B
authors.initials: AB
authors.lastname: Reitz
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D014151:Anti-Anxiety Agents; D001562:Benzimidazoles; D011725:Pyridines