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

B E Maryanoff; S O Nortey; J J McNally; P J Sanfilippo; D F McComsey; B Dubinsky; R P Shank; A B Reitz

doi:10.1016/s0960-894x(99)00240-1

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

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1547-52. doi: 10.1016/s0960-894x(99)00240-1.

Authors

B E Maryanoff¹, S O Nortey, J J McNally, P J Sanfilippo, D F McComsey, B Dubinsky, R P Shank, A B Reitz

Affiliation

¹ Drug Discovery, R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA.

PMID: 10386933
DOI: 10.1016/s0960-894x(99)00240-1

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.

MeSH terms

Animals
Anti-Anxiety Agents / chemical synthesis*
Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology*
Humans
Inhibitory Concentration 50
Mice
Models, Chemical
Pyridines / chemical synthesis*
Pyridines / pharmacology*
Rats
Structure-Activity Relationship

Substances

Anti-Anxiety Agents
Benzimidazoles
Pyridines