新型PTP 1B抑制剂喹啉腙及酰腙化合物的合成与活性研究  

Syntheses and Activities of Novel Quinohydrazone and Acylhydrazone Compounds as PTP 1B Inhibitors

作　　者：时蕾[1] 杨晓岚 徐晶晶 毕晶晶[1] 张志国[1] 张贵生[1] Shi Lei;Yang Xiaolan;Xu Jingjing;Bi Jingjing;Zhang Zhiguo;Zhang Guisheng(Henan Key Laboratory of Organic Functional Molecules and Drug Innovation,Collaborative Innovation Center of Henan Province for Green Manufacturing of Fine Chemicals,School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang,453007)

机构地区：[1]河南省有机功能分子和药物创新重点实验室,精细化学品绿色制造河南省协同创新中心,河南师范大学化学化工学院,新乡453007

出　　处：《化学通报》2021年第1期81-89,共9页Chemistry

基　　金：河南省自然科学基金项目(182300410131);国家自然科学基金项目(21702051,21772032);河南省博士后科研基金项目(001802033)资助。

摘　　要：喹啉腙及喹啉酰腙类化合物具有广泛的生物活性。本文设计合成了29个未见报道的4-(2-芳基)喹啉芳腙和芳酰腙类化合物,采用光吸收检测法测试所合成化合物对蛋白酪氨酸磷酸酶PTP 1B的抑制作用。结果表明,喹啉腙类化合物对PTP 1B具有显著的酶抑制作用,在20μg/mL浓度时,有21个化合物对PTP 1B抑制率在80%以上,其中化合物6q的活性(97.98%)最高。因此,这些化合物具有潜在的调节新陈代谢活性,为发展新的抗糖尿病、抗肿瘤药物提供了一定的研究基础。Quinoline hydrazone and quinoline acylhydrazone compounds had been found to have a wide range of biological activities. In this paper, 29 unreported 4-(2-aryl) quinoline arylhydrazone and aroylhydrazone compounds were designed and synthesized, and the inhibitory effects of these compounds on protein tyrosine phosphatase(PTP 1 B) were tested by light absorption detection method. The results showed that quinoline hydrazone compounds have a significant enzyme inhibitory effect on PTP 1 B. At the concentration of 20 μg/mL, 21 as-synthesized compounds have an inhibition rate of over 80% for PTP 1 B. Among them, compound 6 q has the best inhibitory rate of 97.98%. Therefore, these compounds have the potential to regulate metabolism, and provide a certain research basis for the development of new anti-diabetes and anti-tumor drugs.

关 键 词：喹啉衍生物 腙 酰腙 PTP 1B 

分 类 号：TQ460.1[化学工程—制药化工]