Synthesis of Pyrazolo[۱,۲-b]phthalazine-۵,۱۰-dione Derivatives: A New Class of α –Glucosidase Inhibitors
- سال انتشار: 1399
- محل انتشار: مجله تحقیقات دارویی و بیومدیک، دوره: 7، شماره: 2
- کد COI اختصاصی: JR_PBRE-7-2_007
- زبان مقاله: انگلیسی
- تعداد مشاهده: 46
نویسندگان
Department of chemistry, Payame Noor University (PNU), P.O Box ۱۹۳۹۵-۴۶۹۷, Tehran,Iran.
Department of chemistry, Payame Noor University (PNU), P.O Box ۱۹۳۹۵-۴۶۹۷, Tehran,Iran.
Department of Biomaterials, The Institue of Pharmaceutical Sciences(TIPS), Tehran University of Medical Sciences, Tehran, Iran.
Department of Medicinal Chemistry, Development Research Center, School of Pharmacy, and Drug Design, Tehran University of Medical Sciences, Tehran, Iran.
چکیده
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[۱,۲-b]phthalazine-۵,۱۰-dione derivatives ۵a–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 (EC۳.۲.۱.۲۰, Saccharomyces cerevisiae) at ۲۰ U/mg concentration. Results: Four compounds showed higher α-glucosidase inhibitory activity in comparison to a standard, i.e., Acarbose. Compound ۵q displays the most potent α-glucosidase inhibitory activity (IC۵۰ = ۱۵۵.۴ ± ۶.۰ 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.کلیدواژه ها
α-Glucosidase inhibitors, Pyrazolophthalazine, Malononitrile, Aldehydeاطلاعات بیشتر در مورد COI
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