Pyrazole scaffold-based derivatives: A glimpse of α-glucosidase inhibitory activity, SAR, and route of synthesis

被引:10
作者
ul Firdaus, Jannat [1 ]
Siddiqui, Nadeem [1 ,3 ]
Alam, Ozair [1 ,3 ]
Manaithiya, Ajay [1 ]
Chandra, Kailash [2 ]
机构
[1] Jamia Hamdard, Sch Pharmaceut Educ & Res, Dept Pharmaceut Chem, Med Chem & Mol Modelling Lab, New Delhi, India
[2] Jamia Hamdard, Hamdard Inst Med Sci & Res, Dept Biochem, New Delhi, India
[3] Jamia Hamdard, Sch Pharmaceut Educ & Res, Dept Pharmaceut Chem, Med Chem & Mol Modelling Lab, New Delhi 110062, India
关键词
alpha-glucosidase inhibitors; biological activity; docking study; pyrazole; structure-activity relationship; INTESTINAL MALTASE-GLUCOAMYLASE; BIOLOGICAL EVALUATION; SUBSTRATE-SPECIFICITY; EFFICIENT SYNTHESIS; MOLECULAR DOCKING; AMYLASE; DESIGN; MECHANISM; HOMOLOGY; MIGLITOL;
D O I
10.1002/ardp.202200421
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The alpha-glucosidase is a validated target to develop drugs for treating type 2 diabetes mellitus. The existing alpha-glucosidase inhibitors have certain shortcomings related to side effects and route of synthesis. Accordingly, it is inevitable to develop new chemical templates as alpha-glucosidase inhibitors. Pyrazole derivatives have a special place in medicinal chemistry because of various biological activities. Recently, pyrazole-based heterocyclic compounds have emerged as a promising scaffold to develop alpha-glucosidase inhibitors. This study focuses on the recently reported pyrazole-based alpha-glucosidase inhibitors, including their biological activity (in vivo, in vitro, and in silico), structure-activity relationship, and ways of synthesis. The literature revealed the development of several promising pyrazole-based alpha-glucosidase inhibitors and new synthetic routes for their preparation. The encouraging alpha-glucosidase inhibitory results of the pyrazole-based heterocyclic compounds make them an attractive target for further research. The authors also foresee the arrival of the pyrazole-based alpha-glucosidase inhibitors in clinical practice.
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页数:28
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