Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2- α]benzimidazoles

Article abstract of DOI:10.1016/S0960-894X(99)00240-1

A variety of pyrido[1,2-α]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.