1,2,4-三氮唑和哌嗪的酰胺类化合物的合成及生物活性

Synthesis and Biological Activities of Amide Derivatives Containing 1,2,4-Tiazole and Piperazine

以氨基硫脲、芳甲酰卤为原料,经亲核取代、环化、亲核取代3步反应制得5-芳基-1,2,4-三氮唑-2-巯基乙酸后,再与单芳酰基哌嗪缩合合成18个未见文献报道的含1,2,4-三氮唑环的双取代哌嗪衍生物。目标化合物的结构通过1HNMR、IR、MS和HRMS确认。初步生物活性测试表明:目标化合物具有一定的抗肿瘤活性。

2-（5-Aryl-4H-1,2,4-triazol-3-yhhio） acetic acid synthesized from aromatic formyl halide and thiosemicarbazide used as raw materials via nucleophilic substitution reaction, alkylotion reaction, nucleophilic substitution reaction. Finally, 18 disubstitutedpiperazine derivatives containing a 1,2,4-triazole ring were synthesized by the reaction of 2-（5-aroyl-4H- 1,2, 4-triazol-3-yhhio） acetic acid with mono substituted aroyl piperazine. The structures of all compounds have been confirmed by 1HNMR,IR, MS and HRMS. Preliminary bioas- say results indicated that compounds exhibited anticancer activity.