Synthesis and Anticonvulsant Activity of Certain N-Aralkyl- N-(1-Substituted Cyclohexyl) Benzenamines
作者:M. Nabil Aboul-Enein
DOI:10.3797/scipharm.2006.74.1
日期:——
The synthesis of certain N-aralkyl(1-aminomethylcyclohexyl) benzenamines 6a-i, N-(alkyloxymethyl or aralkyloxymethylcyclohexyl)-N-arylbenzenamines 9a-l and 1-(1-(aralkylphenylamino)cyclohexyl methoxy)-3-isopropylaminopropan-2-ols 11a-c has been accomplished. These compounds exhibited anticonvulsant activity. Compounds 9h, 9b and 11a at doses 0.06, 0.075 and 0.08 mmol/kg, respectively provoked maximal anticonvulsant potential against pentylenetetrazol (PTZ) induced seizures test compared with diphenylhydantoin (0.2 mmol/kg) and valproic acid (0.24mmol/kg).
已合成某些N-aralkyl(1-aminomethylcyclohexyl)苯胺6a-i,N-(烷氧基甲基或芳烷氧基甲基环己基)-N-芳基苯胺9a-l以及1-(1-(芳烷基苯胺)环己基甲氧基)-3-异丙胺丙醇-2-醇11a-c。这些化合物表现出抗惊厥活性。化合物9h、9b和11a在剂量0.06、0.075和0.08 mmol/kg下,对小鼠应用戊烷四唑(PTZ)诱导的惊厥测试展现出最大的抗惊厥潜力,相较于苯二氮卓(0.2 mmol/kg)和丙戊酸(0.24mmol/kg)。