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基于发作性睡病治疗药物莫达非尼的结构,设计并合成了两个系列的新化合物,分别为2-[(二苯甲基)亚砜基]乙酰胺类和2-[(二苯甲基)硫代]乙酰胺类化合物,并测定了这些化合物的生物活性。以二苯基甲醇为原料,经取代、氧化和酰化等反应合成了15个目标化合物(6a～6o),其结构经ESI-MS、1H NMR和元素分析确证。以小鼠自主活动实验测定了合成化合物对小鼠中枢神经的影响。初步构效关系表明,化合物6c、6f、6h和6n能提高小鼠的自主活动,其中6h的中枢兴奋活性略强于阳性对照药莫达非尼。
Based on the structure of modafinil, a therapeutic drug for narcolepsy, two series of new compounds were designed and synthesized, which are 2 - [(diphenylmethyl) sulfoxide] acetamide and 2 - [ Methyl) thio] acetamides, and the biological activities of these compounds were determined. Fifteen target compounds (6a ~ 6o) were synthesized through the reaction of substitution, oxidation and acylation with diphenylmethanol as raw materials. The structures of the target compounds were confirmed by ESI-MS, 1H NMR and elemental analysis. The effects of the synthesized compounds on the central nervous system of mice were determined by mouse autonomic activity. The preliminary structure-activity relationship showed that compounds 6c, 6f, 6h and 6n increased autonomic activity in mice, of which the 6h central excitation activity was slightly stronger than the positive control drug modafinil.