Title of article
Potential Anxiolytic Agents. Part 4: Novel Orally-Active N5-Substituted Pyrido[1,2-a]benzimidazoles with High GABA-A Receptor Affinity
Author/Authors
Alfonzo D. Jordan، نويسنده , , Anil H. Vaidya، نويسنده , , Daniel I. Rosenthal، نويسنده , , Barry Dubinsky، نويسنده , , Cheryl P. Kordik، نويسنده , , Pauline J. Sanfilippo and، نويسنده , , Wu-Nan Wu، نويسنده , , Allen B. Reitz، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
6
From page
2381
To page
2386
Abstract
A series of pyrido[1,2-a]benzimidazoles (PBIs) with substitution on the N5-nitrogen has been synthesized and found to possess high affinity for the benzodiazepine (BZD) site on the GABA-A receptor. The compounds evaluated include those bearing a heteroalkyl group and heterocyclic rings. The most promising of these compounds is ethoxymethyl analogue 24, which has an IC50 of 0.1 nM for the BZD site on the GABA-A receptor and has been advanced to human clinical trials.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792453
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