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، جلد ۷، شماره ۲، صفحات ۱۲۱-۱۳۲
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| عنوان فارسی |
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| چکیده فارسی مقاله |
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| کلیدواژه‌های فارسی مقاله |
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| عنوان انگلیسی |
Synthesis of Pyrazolo[1,2-b]phthalazine-5,10-dione Derivatives: A New Class of α –Glucosidase Inhibitors |
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| چکیده انگلیسی مقاله |
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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| کلیدواژه‌های انگلیسی مقاله |
α-Glucosidase inhibitors, Pyrazolophthalazine, Malononitrile, Aldehyde |
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| نویسندگان مقاله |
| Maryam Hosseinpoor Tehrani
Department of chemistry, Payame Noor University (PNU), P.O Box 19395-4697, Tehran,Iran.
| Seyed Ahmad Mirshokraie
Department of chemistry, Payame Noor University (PNU), P.O Box 19395-4697, Tehran,Iran.
| Mehdi Khoobi
Department of Biomaterials, The Institue of Pharmaceutical Sciences(TIPS), Tehran University of Medical Sciences, Tehran, Iran.
| Mohsen Amini
Department of Medicinal Chemistry, Development Research Center, School of Pharmacy, and Drug Design, Tehran University of Medical Sciences, Tehran, Iran.
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| نشانی اینترنتی |
http://pbr.mazums.ac.ir/browse.php?a_code=A-10-718-1&slc_lang=en&sid=1 |
| فایل مقاله |
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| کد مقاله (doi) |
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| زبان مقاله منتشر شده |
en |
| موضوعات مقاله منتشر شده |
شیمی دارویی |
| نوع مقاله منتشر شده |
پژوهشی |
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