7,8-METHYLENEDIOXY-4H-2,3-BENZODIAZEPIN-4-ONES AS NOVEL AMPA RECEPTORANTAGONISTS

Authors
DESARRO A DESARRO G GITTO R GRASSO S MICALE N QUARTARONE S ZAPPALA M
Citation
A. Desarro et al., 7,8-METHYLENEDIOXY-4H-2,3-BENZODIAZEPIN-4-ONES AS NOVEL AMPA RECEPTORANTAGONISTS, Bioorganic & medicinal chemistry letters, 8(8), 1998, pp. 971-976
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
8
Year of publication
1998
Pages
971 - 976
Database
ISI
SICI code
0960-894X(1998)8:8<971:7ANAR>2.0.ZU;2-I
Abstract
The synthesis and anticonvulsant activity of novel 7,8-methylenedioxy- 4H-2,3-benzodiazepin-4-ones 3a-e, structurally-related to GYKI 52466 1 , a well-known noncompetitive AMPA-receptor antagonist, are reported. The new compounds possess marked anticonvulsant properties and, in ana logy to 1, antagonize seizures induced by AMPA. In addition, when comp ared to the model compound 1, compounds 3 show a longer-lasting antico nvulsant activity and a lower toxicity. (C) 1998 Elsevier Science Ltd. All rights reserved.