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目的设计并合成芳酰胺基噻唑类衍生物,测定其体外对CCR4的趋化抑制作用,期望发现结构新颖的CCR4小分子抑制剂。方法以1,3-二氯丙酮和硫脲为起始原料,经5步反应制得目标化合物;采用Boyden小室法研究目标化合物对巨噬细胞源趋化因子(MDC)通过CCR4所介导的趋化HEK293细胞的抑制作用。结果与结论合成了11个未见文献报道的新化合物,其结构均经核磁共振氢谱和质谱确证。生物活性初步评价结果显示,该类化合物对CCR4细胞趋化作用具有一定的抑制作用。
OBJECTIVE To design and synthesize arylaminothiazole derivatives and determine their chemotactic inhibitory effect on CCR4 in vitro. It is expected to find new structural inhibitors of CCR4. METHODS: 1,3-Dichloroacetone and thiourea were used as starting materials to prepare the target compounds in five steps. The targeted compounds were investigated by Boyden chamber method for the effect of macrocyte-derived chemokines (MDC) on CCR4 Chemotaxis of HEK293 cells. RESULTS AND CONCLUSIONS A total of 11 new compounds were synthesized and their structures were confirmed by 1H-NMR and MS. Preliminary evaluation of biological activity results show that these compounds have a certain inhibition of chemotaxis of CCR4 cells.