Pharmaceutical and Biomedical Research

en Synthesis of Pyrazolo[1,2-b]phthalazine-5,10-dione Derivatives: A New Class of α –Glucosidase Inhibitors شیمی دارویی Medical Chemistry پژوهشي Original Research <div style="text-align: justify;">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. </div> α-Glucosidase inhibitors, Pyrazolophthalazine, Malononitrile, Aldehyde 121 132 http://pbr.mazums.ac.ir/browse.php?a_code=A-10-718-1&slc_lang=en&sid=1 Maryam Hosseinpoor Tehrani m250_tehrani@yahoo.com 10031947532846006657 10031947532846006657 No Department of chemistry, Payame Noor University (PNU), P.O Box 19395-4697, Tehran,Iran. Seyed Ahmad Mirshokraie a.mirshokraie@gmail.com 10031947532846006658 10031947532846006658 No Department of chemistry, Payame Noor University (PNU), P.O Box 19395-4697, Tehran,Iran. Mehdi Khoobi mehdi.khoobi@gmail.com 10031947532846006659 10031947532846006659 No Department of Biomaterials, The Institue of Pharmaceutical Sciences(TIPS), Tehran University of Medical Sciences, Tehran, Iran. Mohsen Amini moamini@tums.ac.ir 10031947532846006660 10031947532846006660 Yes Department of Medicinal Chemistry, Development Research Center, School of Pharmacy, and Drug Design, Tehran University of Medical Sciences, Tehran, Iran.