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新型抗癫痫药物的研制。III. 1-(对-氨磺酰苯基)-咪唑烷酮-5的某些衍生物的抗惊厥活性(作者译)

[Development of new antiepileptic agents. III. Anticonvulsant activity of some derivatives of 1-(p-sulfamoylphenyl)-imidazolidinone-5 (author's transl)].

作者信息

Waser P G, Ganz A J, Pfirrmann R W

出版信息

Arzneimittelforschung. 1977;27(12):2336-41.

PMID:580046
Abstract

A series of derivatives of 1-(p-sulfamoylphenyl)imidazolidinone-5 were tested for anticonvulsant properties against electroshock and pentylenetetrazole seizures. They were also screened for analgesic, sedative and toxic effects. The substances that had the best anticonvulsant activities were those with halogen substitution in the ortho position of the 1-phenylring of 1-(p-sulfamoylphenyl)-3-phenylimidazolidinone-5. Additional substitutions on the basic structure (imidazolidinone-5) or on the 3-phenylring diminished the anticonvulsant activity. The anticonvulsants are less toxic than diphenylhydantoin. Some of the substances exhibited feeble analgesic and sedative properties.

摘要

对一系列1-(对氨磺酰基苯基)咪唑烷酮-5的衍生物进行了抗惊厥特性测试,以对抗电休克和戊四氮惊厥。还对它们进行了镇痛、镇静和毒性作用的筛选。具有最佳抗惊厥活性的物质是那些在1-(对氨磺酰基苯基)-3-苯基咪唑烷酮-5的1-苯环邻位有卤素取代的物质。在基本结构(咪唑烷酮-5)或3-苯环上的额外取代会降低抗惊厥活性。这些抗惊厥药的毒性比苯妥英低。其中一些物质表现出微弱的镇痛和镇静特性。

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