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
1996.0

Abstract

We have further explored the structure-activity relationships of pyrido[1,2-a]benzimidazole (PBI) derivatives (viz. prototype 1), a novel series of central GABA-A receptor modulators, with the intent of enhancing oral efficacy. A study involving the introduction of acidic or basic groups led to the identification of RWJ-38293 (3a) as a potential anxiolytic agent.

Knowledge Graph

Similar Paper

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 1996.0
Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles
Bioorganic & Medicinal Chemistry Letters 1999.0
Potential Anxiolytic Agents. Pyrido[1,2-a]benzimidazoles: A New Structural Class of Ligands for the Benzodiazepine Binding Site on GABA-A Receptors
Journal of Medicinal Chemistry 1995.0
Potential Anxiolytic Agents. Part 4: Novel Orally-Active N5-Substituted Pyrido[1,2-a]benzimidazoles with High GABA-A Receptor Affinity
Bioorganic & Medicinal Chemistry Letters 2002.0
Discovery of Imidazo[1,2-b][1,2,4]triazines as GABA<sub>A</sub> α2/3 Subtype Selective Agonists for the Treatment of Anxiety
Journal of Medicinal Chemistry 2006.0
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4- triazol-3-ylmethoxy)-3-(2-fluorophenyl)- 1,2,4-triazolo[4,3-b]pyridazine:  A Functionally Selective γ-Aminobutyric Acid<sub>A</sub>(GABA<sub>A</sub>) α2/α3-Subtype Selective Agonist That Exhibits Potent Anxiolytic Activity but Is Not Sedating in Animal Models
Journal of Medicinal Chemistry 2005.0
Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABA<sub>A</sub>α2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders
Journal of Medicinal Chemistry 2006.0
Synthesis, Pharmacology, and Structure−Activity Relationships of Novel Imidazolones and Pyrrolones as Modulators of GABA<sub>A</sub>Receptors
Journal of Medicinal Chemistry 2006.0
Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands
Bioorganic &amp; Medicinal Chemistry 2017.0
Identification of a New Pyrazolo[1,5-a]quinazoline Ligand Highly Affine to γ-Aminobutyric Type A (GABA<sub>A</sub>) Receptor Subtype with Anxiolytic-Like and Antihyperalgesic Activity
Journal of Medicinal Chemistry 2017.0