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1-芳基-6,7-亚甲基二氧基-3H-喹唑啉-4-酮作为抗惊厥剂

1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents.

作者信息

Zappalà Maria, Grasso Silvana, Micale Nicola, Zuccalà Giuseppe, Menniti Frank S, Ferreri Guido, De Sarro Giovambattista, De Micheli Carlo

机构信息

Dipartimento Farmaco-Chimico, Università di Messina, viale Annunziata, 98168 Messina, Italy.

出版信息

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4427-30. doi: 10.1016/j.bmcl.2003.09.032.

DOI:10.1016/j.bmcl.2003.09.032
PMID:14643339
Abstract

A set of novel 1-aryl-6,7-methylenedioxy-3H-quinazolin-4-(thi)ones (3a-f) has been designed and screened as anticonvulsant agents in DBA/2 mice. The new compounds are provided with anticonvulsant properties comparable to those of GYKI 52466. To clarify the mode of action, their affinity for the quinazolinone/2,3-benzodiazepine site of the AMPA receptor complex has been assayed.

摘要

设计并筛选了一组新型的1-芳基-6,7-亚甲基二氧基-3H-喹唑啉-4-（硫）酮（3a-f），作为DBA/2小鼠的抗惊厥剂。这些新化合物具有与GYKI 52466相当的抗惊厥特性。为了阐明其作用方式，已测定了它们对AMPA受体复合物喹唑啉酮/2,3-苯并二氮杂䓬位点的亲和力。

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