Volume 7, Issue 2 (2021)                   Pharm Biomed Res 2021, 7(2): 121-132 | Back to browse issues page


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Hosseinpoor Tehrani M, Mirshokraie S A, Khoobi M, Amini M. Synthesis of Pyrazolo[1,2-b]phthalazine-5,10-dione Derivatives: A New Class of α –Glucosidase Inhibitors. Pharm Biomed Res. 2021; 7 (2) :121-132
URL: http://pbr.mazums.ac.ir/article-1-253-en.html
1- Department of chemistry, Payame Noor University (PNU), P.O Box 19395-4697, Tehran,Iran.
2- Department of Biomaterials, The Institue of Pharmaceutical Sciences(TIPS), Tehran University of Medical Sciences, Tehran, Iran.
3- Department of Medicinal Chemistry, Development Research Center, School of Pharmacy, and Drug Design, Tehran University of Medical Sciences, Tehran, Iran.
Abstract:   (3050 Views)
Background: Hyperglycemia is a metabolic disorder that refers to an increase in blood sugar in diabetic patients. α-Glucosidase has been introduced as a membrane-bound enzyme, and it is the main enzyme for carbohydrate digestion in some parts of the intestine. Inhibition of α -glucosidase enzyme activity is a reliable approach to control post-prandial hyperglycemia condition.
Objectives: In this study, a series of Pyrazolo[1,2-b]phthalazine-5,10-dione derivatives 5a–t were synthesized via a multicomponent reaction and evaluated as new inhibitors for α-glucosidase.
Methods: The biological activity of the synthesized compounds was studied using a source of the α-glucosidase enzyme (EC3.2.1.20, Saccharomyces cerevisiae) at 20 U/mg concentration. 
Results: Four compounds showed higher α-glucosidase inhibitory activity in comparison to a standard, i.e., Acarbose. Compound 5q displays the most potent α-glucosidase inhibitory activity (IC50 = 155.4 ± 6.0 μM). 
Conclusion: In conclusion, some of the synthesized compounds, including heterocyclic core molecules, have shown remarkable activity that could be considered as subjects for the development of new, more efficient inhibitors of the α-glucosidase enzyme. 
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Type of Study: Original Research | Subject: Medical Chemistry

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