Calis U, Dalkara S, Ertan M
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Arzneimittelforschung. 1992 May;42(5):592-4.
In this study, some new 4-aryl-4-imidazoline-2-one derivatives have been prepared by the reaction of potassium cyanate with some aminoethanone hydrochlorides. The structure of these compounds have been confirmed by UV, IR, 1H-NMR and elementary analysis. Their anticonvulsant activities were determined by maximal electroshock (MES) and subcutaneous metrazol (ScMet) tests according to the ADD (Antiepileptic Drug Development) programme Phase I. Neurotoxicity of the compounds was evaluated by rotarod test. While 2 of the compounds showed protection against ScMet induced seizures at 30 and 300 mg/kg dose levels, 3 of the compounds showed neurotoxicity.
在本研究中，通过氰酸钾与一些氨基乙酮盐酸盐的反应制备了一些新的4-芳基-4-咪唑啉-2-酮衍生物。这些化合物的结构已通过紫外光谱（UV）、红外光谱（IR）、核磁共振氢谱（1H-NMR）和元素分析得以确证。根据抗癫痫药物开发（ADD）计划第一阶段，通过最大电休克（MES）和皮下注射戊四氮（ScMet）试验测定了它们的抗惊厥活性。通过转棒试验评估了这些化合物的神经毒性。虽然其中2种化合物在30和300mg/kg剂量水平下对ScMet诱导的癫痫发作具有保护作用，但有3种化合物表现出神经毒性。
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