Verma Manjusha, Pandeya Surendra Nath, Singh Krishna Nand, Stables James P
Department of Applied Chemistry, Institute of Technology, Banaras Hindu University, Varanasi-221005, India.
Acta Pharm. 2004 Mar;54(1):49-56.
Schiff bases of N-methyl and N-acetyl isatin derivatives with different aryl amines have been synthesized and screened for anticonvulsant activities against maximal electroshock (MES) and subcutaneous metrazole (ScMet). N-methyl-5-bromo-3-(p-chlorophenylimino) isatin (2) exhibited anticonvulsant activity in MES and ScMet with LD50 > 600 mg kg(-1), showing better activity than the standard drugs phenytoin, carbamazepine and valproic acid. Thus, compound 2 may be chosen as a prototype for development of new anticonvulsants.
已合成了N-甲基和N-乙酰异吲哚酮衍生物与不同芳基胺的席夫碱，并针对最大电休克（MES）和皮下注射戊四氮（ScMet）进行了抗惊厥活性筛选。N-甲基-5-溴-3-（对氯苯基亚氨基）异吲哚酮（2）在MES和ScMet试验中表现出抗惊厥活性，半数致死量（LD50）>600 mg kg⁻¹，显示出比标准药物苯妥英、卡马西平和丙戊酸更好的活性。因此，化合物2可被选为开发新型抗惊厥药物的原型。
