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
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container_issue 14
container_start_page 1953
container_title Bioorganic & medicinal chemistry letters
container_volume 9
creator Anderson, B A
Harn, N K
Hansen, M M
Harkness, A R
Lodge, D
Leander, J D
description 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.
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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects 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
title Synthesis and anticonvulsant activity of 3-aryl-5H-2,3-benzodiazephine AMPA antagonists
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