1. 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
- Author
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Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, and Urwyler S
- Subjects
- Administration, Oral, Animals, Anticonvulsants administration & dosage, Anticonvulsants chemistry, Crystallography, X-Ray, Disease Models, Animal, Dose-Response Relationship, Drug, Mice, Mice, Inbred DBA, Models, Molecular, Molecular Structure, Quinazolinones administration & dosage, Quinazolinones chemistry, Seizures drug therapy, Stereoisomerism, Structure-Activity Relationship, Sulfonamides administration & dosage, Sulfonamides chemistry, Anticonvulsants pharmacology, Quinazolinones pharmacology, Receptors, AMPA antagonists & inhibitors, Sulfonamides pharmacology
- Abstract
A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage., (Copyright © 2011. Published by Elsevier Ltd.)
- Published
- 2012
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