Synthesis and anticonvulsant activity of 1-substituted benzyl-N-substituted-1, 2, 3-triazo

Synthesis and anticonvulsant activity of 1-substituted benzyl-N-substituted-1, 2, 3-triazole-4-for-mamides

WANG Junmin;JUN Changsoo;CHAI Kyuyun;KWAK Kyungchell;QUAN Zheshan

【期刊名称】《自然科学进展（英文版）》 【年(卷),期】2006(016)009

【摘要】Substituted benzyl azids were synthesized through the reaction of substituted benzyl chloride and sodium azid, which subsequently underwent cyclization with ethyl propiolate and amidation to give thirteen

1-substituted

benzyl-N-substituted-1,

2,

3-triazole-4-

formamide derivatives (3a-3m). The structure of the synthesized compounds was confirmed by IR, 1H-NMR, MS and elemental analysis. Their anticonvulsant activity against maximal electrolshock (MES) induced seizure was tested and the result showed that all these compounds possess anticonvulsant activity in different degrees. Among those, the compounds containing chloro atoms on the phenyl ring were less potent in anticonvulsant activity, while introducing one or two fluorin atoms on benzyl system increased its activity. Furthermore, their activity decreased when there was substituent on the nitrogen atom of carboxamide, and the larger the substituent, the lower the activity. 【总页数】5页(925-929)

【关键词】1-substituted benzyl-N-substituted-1,2, 3-triazole-4-