作者:Henryk Marona、Elżbieta Pękala、Lucyna Antkiewicz-Michaluk、Maria Walczak、Edward Szneler
DOI:10.1016/j.bmc.2008.06.039
日期:2008.8
A series of appropriate alkanolamine and amide derivatives of xanthone were prepared and evaluated for anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) induced seizures, and for neurotoxicity (TOX) using the rotorod test on mice and rats. The most promising compounds seem to be the appropriate aminoalkanolic derivatives of 6-chloroxanthone, among
制备了一系列合适的of吨酮链烷醇胺和酰胺衍生物,并通过最大电击(MES)和皮下戊四氮(scMet)诱发的癫痫发作评估了其抗惊厥活性,并使用了Rotorod试验对小鼠和大鼠进行了神经毒性(TOX)评估。最有前途的化合物似乎是6-氯吨蒽酮的合适氨基烷基衍生物,其中6-氯-2-甲基黄酮的R-(-)和S-(+)-2氨基-1-丙醇衍生物(2(a)和2(b))表现出抗MES活性(在小鼠中),保护指数(TD(50)/ ED(50))为6.23 <6.85,与苯妥英钠,卡马西平和丙戊酸盐相对应。通过使用放射性配体结合测定法,确定活性最高的化合物2(b)对苯二氮卓(BDZ)受体和电压依赖性Ca(2+)通道(VDCC)具有亲和力。