Hybrid Pyrazole-Tetrazole Derivatives with High α-Amylase Inhibition Activity: Synthesis, Biological Evaluation and Docking Study

被引:9
作者
Harit, Tarik [1 ]
Cherfi, Mounir [1 ]
Daoudi, Nour Elhouda [2 ]
Isaad, Jalal [3 ]
Bnouham, Mohamed [2 ]
Malek, Fouad [1 ]
机构
[1] Mohamed 1st Univ, Fac Sci, Lab Appl Chem & Environm ECOMP, BP 717, Oujda 60000, Morocco
[2] Mohamed 1st Univ, Fac Sci, Lab Bioresources Biotechnol Ethnopharmacol & Hlth, Oujda 60000, Morocco
[3] Abdelmalek Essaadi Univ, FSTH, ERCI2 A, Tetouan 93000, Morocco
关键词
alpha-Amylase; Docking; Pyrazole; Tetrazole; Structure activity relationship; GLUCOSIDASE; MECHANISM; ACARBOSE;
D O I
10.1002/slct.202203757
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The elaboration of some N-alkylated pyrazole-tetrazole derivatives is reported. The structures of the newly ones are verified using NMR and FTIR spectroscopies, mass spectrometry as well as elemental analysis. Their potencies to inhibit the alpha-amylase enzyme were evaluated using spectrophotometric method and the obtained results showed that some of them were extremely potent with respect to the used positive control. The structure activity relationship showed that the alpha-amylase inhibition activity depends on the alkylation position as well as the nature of the alkyl moiety and the alkylation at the N1 position with a donor group improves the alpha-amylase inhibition activity. Docking study was also performed and the obtained results support the experimental results in the case of the alkylation position effect. These findings suggest that the molecules reported in this study may be used as good drug candidate to treat Type 2 diabetes.
引用
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页数:7
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