RT - Journal Article T1 - Synthesis of Pyrazolo[1,2-b]phthalazine-5,10-dione Derivatives: A New Class of α –Glucosidase Inhibitors JF - mazums-pbr YR - 2021 JO - mazums-pbr VO - 7 IS - 2 UR - http://pbr.mazums.ac.ir/article-1-253-en.html SP - 121 EP - 132 K1 - α-Glucosidase inhibitors K1 - Pyrazolophthalazine K1 - Malononitrile K1 - Aldehyde AB - 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. LA eng UL http://pbr.mazums.ac.ir/article-1-253-en.html M3 10.18502/pbr.v7i2.7365 ER -