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
Rok vydání:	2010
Předmět:	Benzodiazepine Orally active GABAA receptor medicine.drug_class Chemistry Stereochemistry medicine General Medicine Receptor Anxiolytic agents
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::146135ab445497d0ea0c68ebabc14ecf https://doi.org/10.1002/chin.200251156 Zobrazit plný text záznamu Plný text