European Journal of Chemistry 2017, 8(2), 105-108 | doi: https://doi.org/10.5155/eurjchem.8.2.105-108.1541 | Get rights and content

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Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives


Mohammed El-Fal (1) , Karima Sayah (2) , Ilias Marmouzi (3) , My El Abbes Faouzi (4) , M'hammed Ansar (5) , Jamal Taoufik (6) , El Mokhtar Essassi (7) , Youssef Ramli (8,*)

(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.


Keywords


α-Amylase; IC50 values; α-Glucosidase; Inhibitory activity; 1,3-Dipolarcyclo addition; Pyrazolo[3,4-d]pyrimidine

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DOI: 10.5155/eurjchem.8.2.105-108.1541

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Funding information


Pharmaceutical Laboratories SOTHEMA, Morocco

Citations

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[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
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DOI: 10.1016/j.molstruc.2021.130177
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[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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How to cite


El-Fal, M.; Sayah, K.; Marmouzi, I.; Faouzi, M.; Ansar, M.; Taoufik, J.; Essassi, E.; Ramli, Y. Eur. J. Chem. 2017, 8(2), 105-108. doi:10.5155/eurjchem.8.2.105-108.1541
El-Fal, M.; Sayah, K.; Marmouzi, I.; Faouzi, M.; Ansar, M.; Taoufik, J.; Essassi, E.; Ramli, Y. Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives. Eur. J. Chem. 2017, 8(2), 105-108. doi:10.5155/eurjchem.8.2.105-108.1541
El-Fal, M., Sayah, K., Marmouzi, I., Faouzi, M., Ansar, M., Taoufik, J., Essassi, E., & Ramli, Y. (2017). Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives. European Journal of Chemistry, 8(2), 105-108. doi:10.5155/eurjchem.8.2.105-108.1541
El-Fal, Mohammed, Karima Sayah, Ilias Marmouzi, My El Abbes Faouzi, M'hammed Ansar, Jamal Taoufik, El Mokhtar Essassi, & Youssef Ramli. "Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives." European Journal of Chemistry [Online], 8.2 (2017): 105-108. Web. 28 Nov. 2021
El-Fal, Mohammed, Sayah, Karima, Marmouzi, Ilias, Faouzi, My, Ansar, M'hammed, Taoufik, Jamal, Essassi, El Mokhtar, AND Ramli, Youssef. "Synthesis, and evaluation of α-amylase and α-glucosidase inhibitory potential of new pyrazolo[3,4-d]pyrimidine derivatives" European Journal of Chemistry [Online], Volume 8 Number 2 (30 June 2017)

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