title: 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
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.
authors.affiliation: Novartis Institute for Biomedical Research, Global Discovery Chemistry, Basel CH-4002, Switzerland. david.orain@novartis.com
authors.forename: David
authors.initials: D
authors.lastname: Orain
authors.forename: Silvio
authors.initials: S
authors.lastname: Ofner
authors.forename: Manuel
authors.initials: M
authors.lastname: Koller
authors.forename: David A
authors.initials: DA
authors.lastname: Carcache
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Froestl
authors.forename: Hans
authors.initials: H
authors.lastname: Allgeier
authors.forename: Vittorio
authors.initials: V
authors.lastname: Rasetti
authors.forename: Joachim
authors.initials: J
authors.lastname: Nozulak
authors.forename: Henri
authors.initials: H
authors.lastname: Mattes
authors.forename: Nicolas
authors.initials: N
authors.lastname: Soldermann
authors.forename: Philipp
authors.initials: P
authors.lastname: Floersheim
authors.forename: Sandrine
authors.initials: S
authors.lastname: Desrayaud
authors.forename: Joerg
authors.initials: J
authors.lastname: Kallen
authors.forename: Kurt
authors.initials: K
authors.lastname: Lingenhoehl
authors.forename: Stephan
authors.initials: S
authors.lastname: Urwyler
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D051379:Mice; D008811:Mice, Inbred DBA; D008958:Models, Molecular; D015394:Molecular Structure; D052999:Quinazolinones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000188:drug therapy; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000927:Anticonvulsants; D052999:Quinazolinones; D018091:Receptors, AMPA; D013449:Sulfonamides