title: Synthesis and anticonvulsant activity of 3-aryl-5H-2,3-benzodiazephine AMPA antagonists.
abstract: A novel series of 3-aryl-5H-2,3-benzodiazepines with N-3 aromatic substituents has been synthesized. Good in vivo anticonvulsant activity of the new compounds has been demonstrated employing the maximal electroshock seizure test in mice. Evaluation of a subset of the compounds in the cortical wedge assay confirmed the new structures to be AMPA antagonists.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.
authors.forename: B A
authors.initials: BA
authors.lastname: Anderson
authors.forename: N K
authors.initials: NK
authors.lastname: Harn
authors.forename: M M
authors.initials: MM
authors.lastname: Hansen
authors.forename: A R
authors.initials: AR
authors.lastname: Harkness
authors.forename: D
authors.initials: D
authors.lastname: Lodge
authors.forename: J D
authors.initials: JD
authors.lastname: Leander
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004597:Electroshock; D051379:Mice; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / Q000037:antagonists & inhibitors*
chemical_list: D000927:Anticonvulsants; D001569:Benzodiazepines; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; C085266:talampanel