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Research Article | Open Access

New Gemcitabine Derivatives as Potent in vitro α-Glucosidase Inhibitors

Farked Wahoodi Salman1, Ahmed Jasim Twayej2, Hayder Ahmed Shaheed3, Ali Jabbar Radhi3( )
Department of Chemistry, Faculty of Science, Kufa University, Najaf-Iraq
Faculty of Health and Medical Techniques, Al-Kafeel University, Najaf, Iraq
Faculty of Pharmacy, Al-Kafeel University, Najaf, Iraq
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Abstract

In this work, new heterocyclic compounds 1,2,3-triazoline derivatives starting from gemcitabine were synthesized. At first, gemcitabine was converted to 2-azido gemcitabine (G) through the reaction of gemcitabine with sodium azide. 1,2,3-Triazolines were prepared from the reaction of 2-azido gemcitabine with some unsaturated compounds such as malic anhydride, cinamic acid and acryl amide by click reaction. The products were identified by Fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) technique. The α-glucosidase inhibitory activities of all the synthesized compounds were determined in vitro. All the tested compounds showed α-glucosidase inhibitory activity of IC50 = 144.8 ± 1.74, 212.9 ± 3.4 and 345 ± 4.5 μM against the α-glucosidase enzyme when compared to the standard drug acarbose IC50 = 824 ± 1.73 μM.

Keywords

Gemcitabine1,2,3-triazolinesα-glucosidase inhibitors

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Nano Biomedicine and Engineering
Volume 11 Issue 1,
March 2019
Pages 84-90
DOI: 10.5101/nbe.v11i1.p84-90
Cite this article:
Salman FW, Twayej AJ, Shaheed HA, et al. New Gemcitabine Derivatives as Potent in vitro α-Glucosidase Inhibitors. Nano Biomedicine and Engineering, 2019, 11(1): 84-90. https://doi.org/10.5101/nbe.v11i1.p84-90

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Received: 28 June 2018
Accepted: 13 February 2019
Published: 20 March 2019
© Farked Wahoodi Salman, Ahmed Jasim Twayej, Hayder Ahmed Shaheed, and Ali Jabbar Radhi.

This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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