Synthesis and anticonvulsant activity of 3-aryl-5H-2,3-benzodiazephine AMPA antagonists

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-07, Vol.9 (14), p.1953
Hauptverfasser:	Anderson, B A, Harn, N K, Hansen, M M, Harkness, A R, Lodge, D, Leander, J D
Format:	Artikel
Sprache:	eng
Schlagworte:	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid - antagonists & inhibitors Animals Anticonvulsants - chemical synthesis Anticonvulsants - pharmacology Benzodiazepines - chemical synthesis Benzodiazepines - chemistry Benzodiazepines - pharmacology Dose-Response Relationship, Drug Electroshock Mice Seizures - drug therapy Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X