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

Authors
Maryanoff, BE Nortey, SO McNally, JJ Sanfilippo, PJ McComsey, DF Dubinsky, B Shank, RP Reitz, AB
Citation
Be. Maryanoff et al., Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles., BIOORG MED, 9(11), 1999, pp. 1547-1552
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
11
Year of publication
1999
Pages
1547 - 1552
Database
ISI
SICI code
0960-894X(19990607)9:11<1547:PAA3NA>2.0.ZU;2-5
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 di d the 6- and 7-pyrido compounds 3 and 4. (C) 1999 Elsevier Science Ltd. All rights reserved.