二芳(杂)甲硫基乙酰胺类化合物的合成及中枢兴奋活性  

Synthesis and central stimulative activities of diaryl(heteraryl)methanesulfinyl acetamide compounds

作　　者：马殿强[1] 朱雄[2] 张奕华[1] 巫冠中[3] 

机构地区：[1]中国药科大学新药研究中心,南京210009 [2]中国药科大学医药化工研究所,南京210009 [3]中国药科大学药理学教研室,南京210009

出　　处：《中国药科大学学报》2008年第6期481-486,共6页Journal of China Pharmaceutical University

摘　　要：目的:合成二芳(杂)甲硫基乙酰胺类化合物,寻找具有中枢兴奋活性的新型化合物。方法:以异烟酸为原料,经Friedel-Crafts反应、还原、取代、酯化、胺解和氧化等反应合成二芳(杂)甲硫基乙酰胺类化合物(8a～8t)。用小鼠自主活动实验评价其中枢兴奋活性。结果:合成了20个目标化合物,结构经ESI-MS、1H NMR、IR和元素分析确证。药理学实验结果表明,化合物8a、8b和8g能增强健康小鼠的自主活动(P<0.05)。结论:二芳(杂)甲硫基乙酰胺类化合物具有较强的中枢兴奋活性。Aim： To synthesize diaryl（heteraryl） methanesulfinyl acetamide compounds and search for new-type compounds with central stimulative activities. Methods： Target compounds（ 8a-8t） were synthesized starting from isonicotinic acid via Friedel-Crafts reaction, reduction, substitution, esterification, amination and oxidation. Their central stimulative effects were preliminarily evaluated by the independent activity assay in mice. Results： Twenty target compounds were synthesized and their structures were confirmed by ESI-MS, ^1H NMR, IR and elemental analysis. The results of pharmacological test showed that compounds 8a, 8b and 8g enhanced the independent activities of healthy mice （ P 〈 0.05）. Conclusion： Diaryl（heteraryl） methanesulfinyl acetamide compounds possess considerable central stimulative activities.

关 键 词：莫达非尼 硫代乙酰胺 合成 中枢兴奋活性 

分 类 号：TQ463[化学工程—制药化工]