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Synthesis and immunosuppressive activity evaluation of substituted N-imidazolidin-2-ones and N-tetrahydropyrimidin-2(1H)-ones

机译:取代的N-咪唑啉丁-2-酮和N-四氢嘧啶-2(1H)-酮的合成及免疫抑制活性评估

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摘要

Seventeen compounds with either an imidazolin-2-one or a tetrahydropyrimidin-2(1H)-one scaffold were synthesized and evaluated for their immunosuppressive activity in a concanavallin A (ConA)-stimulated mouse splenocytes proliferation test. Three of these molecules exerted a significant activity at 90 μM. All the compounds of the tetrahydropyrimidin-2(1H)-one series have turned out to be inactive showing the crucial role of the imidazolidin-2-one scaffold in the induction of an immunosuppressive activity.
机译:合成了具有咪唑啉-2-酮或四氢嘧啶-2(1H)-1骨架的17种化合物,并在伴刀豆球蛋白A(ConA)刺激的小鼠脾细胞增殖测试中评估了其免疫抑制活性。这些分子中的三个在90μM时发挥了显着的活性。事实证明,四氢嘧啶-2(1H)-一个系列的所有化合物都是无活性的,显示了咪唑啉丁-2-酮骨架在诱导免疫抑制活性中的关键作用。

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