title: Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.
abstract: Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models.
authors.affiliation: Novartis Institutes for BioMedical Research, Global Discovery Chemistry, 4002 Basel, Switzerland. manuel.koller@novartis.com
authors.forename: Manuel
authors.initials: M
authors.lastname: Koller
authors.forename: Kurt
authors.initials: K
authors.lastname: Lingenhoehl
authors.forename: Markus
authors.initials: M
authors.lastname: Schmutz
authors.forename: Ivan-Toma
authors.initials: IT
authors.lastname: Vranesic
authors.forename: Joerg
authors.initials: J
authors.lastname: Kallen
authors.forename: Yves P
authors.initials: YP
authors.lastname: Auberson
authors.forename: David A
authors.initials: DA
authors.lastname: Carcache
authors.forename: Henri
authors.initials: H
authors.lastname: Mattes
authors.forename: Silvio
authors.initials: S
authors.lastname: Ofner
authors.forename: David
authors.initials: D
authors.lastname: Orain
authors.forename: Stephan
authors.initials: S
authors.lastname: Urwyler
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D018360:Crystallography, X-Ray; D051379:Mice; D015394:Molecular Structure; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000927:Anticonvulsants; D052999:Quinazolinones; D018091:Receptors, AMPA; D013449:Sulfonamides