7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists

被引：47
作者：
De Sarro, A
De Sarro, G
Gitto, R
Grasso, S
Micale, N
Quartarone, S
Zappala, M
机构：
[1] Univ Messina, Fac Med, Ist Farmacol, I-98168 Messina, Italy
[2] Univ Catanzaro, Dipartimento Med Sperimentale & Clin, I-88100 Catanzaro, Italy
[3] Univ Messina, Dipartimento Farmaco Chim, I-98168 Messina, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 08期
关键词：
7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones; anticonvulsant activity; AMPA-receptor antagonists;
D O I：
10.1016/S0960-894X(98)00148-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 analogy to 1, antagonize seizures induced by AMPA. In addition, when compared to the model compound 1, compounds 3 show a longer-lasting anticonvulsant activity and a lower toxicity. (C) 1998 Elsevier Science Ltd. All rights reserved.
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收藏
页码：971 / 976
页数：6
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