|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
2
|
|
pubmed:dateCreated |
2001-2-5
|
|
pubmed:abstractText |
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.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jan
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:ChenardB LBL,
pubmed-author:CritchettDD,
pubmed-author:DeVriesK MKM,
pubmed-author:EwingF EFE,
pubmed-author:GanongA HAH,
pubmed-author:GuanowskyVV,
pubmed-author:GuhanSS,
pubmed-author:GuinnM RMR,
pubmed-author:HuangJJ,
pubmed-author:KellyKK,
pubmed-author:LazzaroJJ,
pubmed-author:MennitiF SFS,
pubmed-author:PagnozziM JMJ,
pubmed-author:SeymourP APA,
pubmed-author:StaigersT LTL,
pubmed-author:WelchW MWM
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
22
|
|
pubmed:volume |
11
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
177-81
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:11206453-Animals,
pubmed-meshheading:11206453-Anticonvulsants,
pubmed-meshheading:11206453-Binding, Competitive,
pubmed-meshheading:11206453-Brain,
pubmed-meshheading:11206453-Calcium,
pubmed-meshheading:11206453-Disease Models, Animal,
pubmed-meshheading:11206453-Inhibitory Concentration 50,
pubmed-meshheading:11206453-Isomerism,
pubmed-meshheading:11206453-Neuromuscular Blocking Agents,
pubmed-meshheading:11206453-Protein Binding,
pubmed-meshheading:11206453-Pyridines,
pubmed-meshheading:11206453-Quinazolines,
pubmed-meshheading:11206453-Quinazolinones,
pubmed-meshheading:11206453-Rats,
pubmed-meshheading:11206453-Receptors, AMPA,
pubmed-meshheading:11206453-Seizures,
pubmed-meshheading:11206453-Solubility,
pubmed-meshheading:11206453-Structure-Activity Relationship,
pubmed-meshheading:11206453-Synaptic Transmission
|
|
pubmed:year |
2001
|
|
pubmed:articleTitle |
Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.
|
|
pubmed:affiliation |
Global Research and Development, Groton Laboratories, Pfizer Inc., CT 06340, USA.
|
|
pubmed:publicationType |
Journal Article
|
