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本文通过对已上市的治疗多发硬化症的免疫抑制剂芬戈莫德的结构改造,设计合成了一系列含有二苯醚结构的芬戈莫德类似物。通过体内动物实验对化合物的免疫抑制活性和心脏毒性进行了评价。结果表明,大多数化合物具有一定的免疫抑制活性,其中化合物6c、6d、14c~14e体内免疫抑制活性与阳性药芬戈莫德相当,化合物14e没有心动过缓副作用。
In this paper, a series of analogues of fingolimod containing diphenylether have been designed and synthesized by studying the structural modification of fingolimod, an immunosuppressant that has been marketed to treat multiple sclerosis. The immunosuppressive activity and cardiotoxicity of the compounds were evaluated by in vivo animal experiments. The results showed that most of the compounds had some immunosuppressive activities. The immunosuppressive activities of compounds 6c, 6d and 14c ~ 14e in vivo were comparable to those of fingolimod, a positive drug. Compound 14e had no bradycardia and side effects.