两种缩氨基硫脲衍生物的合成及其生物活性研究  

Synthesis and Bioactivity of Two Thiosemicarbazide Derivatives

作　　者：曾福燃 欧俊言 李培静 庄映芬 游遨[1] 冯安生[1] Zeng Furan;Ou Junyan;Li Peijing;Zhuang Yingfen;You Ao;Feng Ansheng(Department of Environmental Engineering,Guangdong Industry Polytechnic,Guangzhou 510300,China)

机构地区：[1]广东轻工职业技术学院生态环境技术学院,广东广州510300

出　　处：《广东化工》2022年第2期26-28,共3页Guangdong Chemical Industry

基　　金：2020年广东省科技创新战略专项资金项目(pdjh2020b0891);广州市科技计划项目(202102021119);广东省教育厅项目(2020ZDZX2077,2021KTSCX198);广东轻院科研项目(KJRC2020-019,KJ2020-024)。

摘　　要：以4-羟基苯甲醛为起始化合物,通过酯化反应在苯甲醛的羟基位置引入两种不同的酯基,然后在化合物的醛基位置引入氨基硫脲基团,合成2种新型缩氨基硫脲衍生物。所有化合物均通过核磁共振氢谱、碳谱、质谱等进行表征。分别测试这类化合物对酪氨酸酶的抑制活性,结果表明在化合物中引入缩氨基硫脲集团之后,2种化合物对蘑菇酪氨酸酶均表现出良好的抑制效果,其中活性最好的化合物为C1,其对酪氨酸酶的IC;值达到0.8μM,动力学研究表明这类化合物属于竞争型抑制剂。Two new thiosemicarbazide derivatives were synthesized by using 4-hydroxybenzaldehyde as a starting compound, with introducing two different ester groups in the hydroxyl position of benzaldehyde through esterification reaction, following by thiosemicarbazide group in the aldehyde position. All compounds were characterized by 1 H-NMR, 13 C-NMR and MS spectra. And the inhibitory activity of tyrosinase of the compounds were tested. The results showed that the two compounds showed good inhibitory effect on mushroom tyrosinase after the introduction of thiosemicourea group, and the most active compound was C1, whose IC;value of tyrosinase reached 0.8 M. Kinetic study showed that these compounds were competitive inhibitors.

关 键 词：酪氨酸酶抑制剂 缩胺基硫脲衍生物 合成 动力学研究 

分 类 号：TQ[化学工程]