Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (11): 3016-3025.DOI: 10.6023/cjoc201805038 Previous Articles     Next Articles



时蕾, 徐晶晶, 毕晶晶, 张志国, 刘统信, 杨晓岚, 张贵生   

  1. 河南省有机功能分子和药物创新重点实验室 河南师范大学化学化工学院 新乡 453007
  • 收稿日期:2018-05-17 修回日期:2018-06-05 发布日期:2018-07-16
  • 通讯作者: 张贵生
  • 基金资助:


Synthesis and Biological Activity of Benzo[h]quinolinium Hydrazine Compounds

Shi Lei, Xu Jingjing, Bi Jingjing, Zhang Zhiguo, Liu Tongxin, Yang Xiaolan, Zhang Guisheng   

  1. Henan Key Laboratory of Organic Functional Molecules and Drug Innovation, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang 453007
  • Received:2018-05-17 Revised:2018-06-05 Published:2018-07-16
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21605039, 21702051), the Key Scientific Research Project of Henan Provinc (Nos. 18A150009, 17A350006), the Henan Normal University Science Foundation for Young Scholars (No. 2016QK10)

Quinoline derivatives, aryl hydrazines and hydrazide compounds have significant biological activities. Benzo[h] quinoline derivatives were synthesized from 1-naphthylamine, substituted benzaldehyde and methyl pyruvate by Doebner-Miller reaction. After the ester was reduced, the corresponding aldehyde was obtained by oxidation. Benzo[h] quinolinium and quinoline hydrazide compounds were synthesized by reacting benzo[h] quinoline formaldehyde with hydrazine salts and hydrazides, respectively. The preliminary activity data showed that most of the compounds exhibited significant inhibitory activities against cycle protein 25B (CDC 25B) and protein tyrosine phosphatase PTP 1B.

Key words: Benzo[h]quinoline derivatives, hydrazone, hydrazide, CDC 25B, PTP 1B, inhibitory activity