Marona H, Antkiewicz-Michaluk L
Department of Chemical Technology of Drugs Collegium Medicum of the Jagiellonian University, Kraków, Poland.
Acta Pol Pharm. 1998 Nov-Dec;55(6):487-98.
A series of 1,2-aminoalkanol derivatives were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxicity (TOX). Most interesting were the anticonvulsant results of S-(+)-2-amino-1-butanol derivative VIII, which displayed anti-MES activity with a protective index (TD50/ED50) of 4.55 corresponding with that for phenytoin, carbamazepine and valproate.
制备了一系列1,2 -氨基烷醇衍生物，并在最大电休克惊厥（MES）和皮下注射戊四氮惊厥阈值（scMet）试验中评估其抗惊厥活性以及神经毒性（TOX）。最有趣的是S-(+)-2-氨基-1-丁醇衍生物VIII的抗惊厥结果，其显示出抗MES活性，保护指数（TD50/ED50）为4.55，与苯妥英、卡马西平和丙戊酸相当。
