Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity
作者:Arzu Karakurt、Mehmet A. Alagöz、Burcu Sayoğlu、Ünsal Çalış、Sevim Dalkara
DOI:10.1016/j.ejmech.2012.08.037
日期:2012.11
Twenty-three new oxime ester derivatives of nafimidone were synthesized with the prospect of potential anticonvulsant activities. MES and ScM tests were employed for their anticonvulsant activities and rotorod test for neurological deficits. Eighteen compounds were found to be protective against MES seizures. Alkyl (1–8) and arylalkyl (9, 10) oxime ester derivatives were found to be more active than
合成了二十三种新的萘甲酮肟肟衍生物,具有潜在的抗惊厥活性。MES和ScM测试用于其抗惊厥活性,而旋翼仪测试用于神经功能缺损。发现有18种化合物可预防MES发作。烷基(1 - 8)和芳基烷基(9,10)被发现肟酯衍生物为比芳基肟酯衍生物(更积极的11 - 23)。五种化合物(2,3,7,9,10)(在MES测试中在30 mg / kg或更高剂量下于0.5小时起保护作用)显示出最高的活性。在4 h的所有剂量水平下,化合物17是ScM测试中活性最高的化合物。