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Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles
B E Maryanoff1, S O Nortey, J J McNally
1Drug Discovery, R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA.
Bioorganic & Medicinal Chemistry Letters
|July 1, 1999
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.