

Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives
Mohammed El-Fal (1)








(1) Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(2) Laboratories of Pharmacology and Toxicology, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(3) Laboratories of Pharmacology and Toxicology, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(4) Laboratories of Pharmacology and Toxicology, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(5) Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(6) Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(7) Laboratory of Organic Heterocyclic Chemistry URAC 21, Faculty of Sciences, Mohammed V University, 10170, Rabat, Morocco
(8) Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10170, Rabat, Morocco
(*) Corresponding Author
Received: 31 Dec 2016 | Revised: 20 Jan 2017 | Accepted: 11 Feb 2017 | Published: 30 Jun 2017 | Issue Date: June 2017
Abstract
A series of new pyrazolo[3,4-d]pyrimidine compounds were synthesized in excellent yields via sulfuration and 1,3-dipolar cycloaddition and confirmed by MS, FT-IR and NMR techniques. All the prepared compounds were screened in vitro for their α-amylase and α-glucosidase inhibitory activities. Preliminary results indicated that some target compounds exhibited promising α-amylase and α-glucosidase inhibitory activity potency. Among the tested products, the cycloadduct f was found most active inhibitor (IC50 = 134.30 μM) for α-amylase, and the sulphur product b is the most active inhibitor (IC50 = 16.37 μM) for α-glucosidase.
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European Journal of Chemistry
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DOI: 10.5155/eurjchem.8.2.105-108.1541
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Pharmaceutical Laboratories SOTHEMA, Morocco
Citations
[1]. Younes Zaoui, Youssef Ramli, Sang Loon Tan, Edward R.T. Tiekink, Laila Chemlal, Joel T. Mague, Jamal Taoufik, M. E. Abbes Faouzi, M'Hammed Ansar
Synthesis, structural characterisation and theoretical studies of a novel pyridazine derivative: Investigations of anti-inflammatory activity and inhibition of α-glucosidase
Journal of Molecular Structure 1234, 130177, 2021
DOI: 10.1016/j.molstruc.2021.130177

[2]. Mohammed Hussen Bule , Roghaieh Esfandyari, Tadesse Bekele Tafesse, Mohsen Amini, Mohammad Ali Faramarzi, Mohammad Abdollahi
Synthesis, Molecular Docking and α-Glucosidase Inhibitory Activity Study of 2,4,6-triaryl Pyrimidine Derivatives
Letters in Drug Design & Discovery 17(10), 1216, 2020
DOI: 10.2174/1570180817666200103130536

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