从酞嗪二酮中提取的几种新型抗惊厥药。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-11-01 Epub Date: 2012-09-06 DOI:10.1055/s-0032-1323758
M F Zayed, R R Ayyad
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引用次数: 10

摘要

合成了一系列含取代恶二唑的邻苯二酮衍生物X(1-7),并对其抗惊厥活性进行了评价。根据光谱数据和元素分析确定了合成化合物的结构。通过最大电击诱发癫痫(MES)和皮下戊四唑(PTZ)试验评价其抗惊厥活性。所有被测化合物在至少一项抗惊厥试验中显示出相当大的抗惊厥活性。此外,一些被测化合物在MES和PTZ试验中均表现出中度抗惊厥活性。根据这些结果,[3-)2-烷氧羰基甲基硫代二唑-5-基)甲基-6-碘酞-1,4- (2H,3H)-1,4-二酮](X1-7)衍生物可推荐作为新型结构的广谱抗惊厥药。
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Some novel anticonvulsant agents derived from phthalazinedione.

A series of phthalazinedione bearing substituted oxadiazole moiety derivatives X(1-7) were synthesized in good yield and evaluated for their possible anticonvulsant activity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Their anticonvulsant activities were evaluated by the maximal electroshock induced seizure (MES) and subcutaneous pentylenetetrazole (PTZ) tests. All the tested compounds showed considerable anticonvulsant activities in at least one of the anticonvulsant tests. Moreover, some of the tested compounds exhibited moderate anticonvulsant activities in both MES and PTZ tests. From these results,[3-)2-Alkoxycarbonylmethylthioxadiozol-5-yl)methyl -6-Iodophthalazine - 1,4- (2H,3H)-1,4-dion] (X1-7) derivatives could be recommended as novel structures of broad spectrum anticonvulsants.

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