ChemInform Abstract: Potential Anxiolytic Agents. Part 4. Novel Orally-Active N5-Substituted Pyrido[1,2-a]benzimidazoles with High GABA-A Receptor Affinity
Autor: | Daniel I. Rosenthal, Alfonzo D. Jordan, Barry Dubinsky, Allen B. Reitz, Wu-Nan Wu, Pauline J. Sanfilippo, Cheryl P. Kordik, Anil H. Vaidya |
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Rok vydání: | 2010 |
Předmět: | |
Zdroj: | ChemInform. 33 |
ISSN: | 1522-2667 0931-7597 |
Popis: | A series of pyrido[1,2- a ]benzimidazoles (PBIs) with substitution on the N 5 -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 IC 50 of 0.1 nM for the BZD site on the GABA-A receptor and has been advanced to human clinical trials. |
Databáze: | OpenAIRE |
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