Pharmaceutical and Biomedical Research
Pharm Biomed Res
Medical Sciences
http://pbr.mazums.ac.ir
1
admin
2423-4486
2423-4494
10.29252/pbr
8888
en
jalali
1399
11
1
gregorian
2021
2
1
7
2
online
1
fulltext
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;"><strong>Background:</strong> 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.<br>
<strong>Objectives</strong>: 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.<br>
<strong>Methods:</strong> 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. <br>
<strong>Results:</strong> 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). <br>
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.