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Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles
- Source :
- Bioorganic & Medicinal Chemistry Letters. 9:1547-1552
- Publication Year :
- 1999
- Publisher :
- Elsevier BV, 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.
- Subjects :
- Pyridines
Stereochemistry
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
Carboxamide
Ring (chemistry)
Biochemistry
Chemical synthesis
Anxiolytic
Inhibitory Concentration 50
Mice
Structure-Activity Relationship
chemistry.chemical_compound
In vivo
Drug Discovery
medicine
Animals
Humans
Receptor
Molecular Biology
Organic Chemistry
Rats
Anti-Anxiety Agents
Models, Chemical
chemistry
Molecular Medicine
Benzimidazoles
Anxiolytic agents
Derivative (chemistry)
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 9
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....6dd962868c31380af82b842050540140