selurampanel and Seizures

selurampanel has been researched along with Seizures* in 1 studies

Other Studies

1 other study(ies) available for selurampanel and Seizures

Article	Year
Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist. ChemMedChem, 2017, 02-03, Volume: 12, Issue:3 A series of potent quinazolinedione sulfonamide antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor were designed and synthesized. The structure-activity relationships (SAR) and in vivo activity of the series were investigated. In particular, compound 1 S (selurampanel; N-[7-isopropyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1H-quinazolin-3-yl]methanesulfonamide) has shown excellent oral potency against maximal electroshock seizure (MES)-induced generalized tonic-clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy. The X-ray crystal structure of selurampanel bound to the AMPA receptor hGluA was also obtained. Topics: Administration, Oral; Animals; Binding Sites; Binding, Competitive; Crystallography, X-Ray; Disease Models, Animal; Drug Design; Electroshock; Mice; Molecular Dynamics Simulation; Protein Structure, Tertiary; Quinazolinones; Receptors, AMPA; Seizures; Structure-Activity Relationship; Sulfonamides	2017

Article

Year

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist.

ChemMedChem, 2017, 02-03, Volume: 12, Issue:3

A series of potent quinazolinedione sulfonamide antagonists of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor were designed and synthesized. The structure-activity relationships (SAR) and in vivo activity of the series were investigated. In particular, compound 1 S (selurampanel; N-[7-isopropyl-6-(2-methylpyrazol-3-yl)-2,4-dioxo-1H-quinazolin-3-yl]methanesulfonamide) has shown excellent oral potency against maximal electroshock seizure (MES)-induced generalized tonic-clonic seizures in rodents as well as significant activity in patients suffering from various forms of epilepsy. The X-ray crystal structure of selurampanel bound to the AMPA receptor hGluA was also obtained.

Topics: Administration, Oral; Animals; Binding Sites; Binding, Competitive; Crystallography, X-Ray; Disease Models, Animal; Drug Design; Electroshock; Mice; Molecular Dynamics Simulation; Protein Structure, Tertiary; Quinazolinones; Receptors, AMPA; Seizures; Structure-Activity Relationship; Sulfonamides

2017