| Literature DB >> 11206453 |
W M Welch1, F E Ewing, J Huang, F S Menniti, M J Pagnozzi, K Kelly, P A Seymour, V Guanowsky, S Guhan, M R Guinn, D Critchett, J Lazzaro, A H Ganong, K M DeVries, T L Staigers, B L Chenard.
Abstract
Piriqualone (1) was found to be an antagonist of AMPA receptors. Structure activity optimization was conducted on each of the three rings in 1 to afford a series of potent and selective antagonists. The sterically crowded environment surrounding the N-3 aryl group provided sufficient thermal stability for atropisomers to be isolated. Separation of these atropisomers resulted in the identification of (+)-38 (CP-465,022), a compound that binds to the AMPA receptor with high affinity (IC50 = 36 nM) and displays potent anticonvulsant activity.Entities:
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Year: 2001 PMID： 11206453 DOI： 10.1016/s0960-894x(00)00622-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823