Citation: Lei Shi, Xiaolan Yang, Jingjing Xu, Jingjing Bi, Zhiguo Zhang, Guisheng Zhang. Syntheses and Activities of Novel Quinohydrazone and Acylhydrazone Compounds as PTP 1B Inhibitors[J]. Chemistry, ;2021, 84(1): 81-89. shu

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

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

Corresponding author: Guisheng Zhang, zgs@htu.cn
Received Date: 29 May 2020
Accepted Date: 15 June 2020

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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 1B) were tested by light absorption detection method. The results showed that quinoline hydrazone compounds have a significant enzyme inhibitory effect on PTP 1B. At the concentration of 20 μg/mL, 21 as-synthesized compounds have an inhibition rate of over 80% for PTP 1B. Among them, compound 6q 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.
- Quinoline derivatives,
- Hydrazine,
- Hydrazide,
- PTP 1B
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