POTENTIAL ANXIOLYTIC AGENTS .2. IMPROVEMENT OF ORAL EFFICACY FOR THE PYRIDO[1,2-A]BENZIMIDAZOLE (PBI) CLASS OF GABA-A RECEPTOR MODULATORS

Authors
MARYANOFF BE MCCOMSEY DF HO W SHANK RP DUBINSKY B
Citation
Be. Maryanoff et al., POTENTIAL ANXIOLYTIC AGENTS .2. IMPROVEMENT OF ORAL EFFICACY FOR THE PYRIDO[1,2-A]BENZIMIDAZOLE (PBI) CLASS OF GABA-A RECEPTOR MODULATORS, Bioorganic & medicinal chemistry letters, 6(3), 1996, pp. 333-338
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
3
Year of publication
1996
Pages
333 - 338
Database
ISI
SICI code
0960-894X(1996)6:3<333:PAA.IO>2.0.ZU;2-E
Abstract
We have further explored the structure-activity relationships of pyrid o[1,2-a]benzimidazole (PBI) derivatives (viz. prototype 1), a novel se ries of central GABA-A receptor modulators, with the intent of enhanci ng oral efficacy. A study involving the introduction of acidic or basi c groups led to the identification of RWJ-38293 (3a) as a potential an xiolytic agent.