作者:R. Richard Goehring、Thomas D. Greenwood、Jyothi S. Pisipati、James F. Wolfe
DOI:10.1002/jps.2600800818
日期:1991.8
A series of 2-benzylsuccinimides (4a-f) were prepared for evaluation as potential anticonvulsants. Primary (Phase I) screening of these compounds indicated that succinimides 4d and 4e, containing lipophilic (+ pi), electron-withdrawing (+ sigma) phenyl substituents, were the most effective in controlling seizures induced by maximal electroshock (MES) and subcutaneous pentylenetetrazol (scMet). Compounds
制备了一系列的2-苄基琥珀酰亚胺(4a-f)作为潜在的抗惊厥药进行评估。对这些化合物的初步(第一阶段)筛选表明,含有亲脂性(+ pi),吸电子(+ sigma)苯基取代基的琥珀酰亚胺4d和4e是控制最大电击(MES)和皮下戊四氮诱发的癫痫发作最有效的方法(scMet)。化合物4a,4c和4d的抗scMet诱发的癫痫发作活性与其2-苯基琥珀酰亚胺类似物的活性相等,并且在MES测试中更有效。在定量(阶段II)测试中,当通过ip小鼠给药时,通过MES和scMet分析,4d和4e均显示出比原型药物(ethosuximide)更好的抗惊厥潜能。然而,