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目的设计合成一系列(Z)-4-烷基硫基-5-烷基硫基次甲基-1-芳基-3-羟基吡咯酮类化合物,并测定其体内升高白细胞活性。方法以1,3-二氯丙酮为起始原料,与烷基硫醇发生取代反应,再与相应的芳香氨基化合物反应生成席夫碱,使用草酰氯关环,最后与酰氯衍生物酯化得到目标化合物。以赛格力(G-CSF)为阳性对照药物,考察所合成化合物的升高白细胞活性,活性数据以白细胞数和嗜中性粒细胞百分比为依据,同时以小鼠的状态作为初步判断毒性的依据。结果与结论共合成了18个未见文献报道的新化合物,其结构经1H-NMR、MS谱确证。活性测试结果表明,化合物Ⅰ5、Ⅰ16的活性与阳性药相当,具有显著升高白细胞活性。
OBJECTIVE To design and synthesize a series of (Z) -4-alkylthio-5-alkylthiomethyl-1-aryl-3-hydroxypyrrolidones and measure the activity of leukocytes in vivo. Methods 1,3-Dichloroacetone was used as a starting material to react with alkylthiol and react with the corresponding aromatic amino compound to generate Schiff base, which was ring-closed with oxalyl chloride and finally esterified with the acid chloride derivative The target compound. To G-CSF as a positive control drug to investigate the activity of the compounds synthesized by the leukocyte activity, white blood cell count and neutrophil percentage based on the number of mice at the same time as the initial state to determine the toxicity in accordance with. RESULTS AND CONCLUSIONS A total of 18 new compounds were reported in the literature, whose structures were confirmed by 1H-NMR and MS spectra. The results of the activity test showed that the compounds I5 and I16 have the same activity as the positive drug and have remarkably increased leukocyte activity.