Abstract
In vitro evaluation of alpha-amylase inhibition was carried out using novel representatives of sulfanyl-substituted azoles such as 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1H-pyrazole) (1), 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1H-pyrazole)·2HCl (2), 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1,2-isoxazole) (3), and 4-(phenylsulfanylmethyl)-3,5-dimethyl-1H-pyrazole (4). The inhibition of alpha-amylase with compound (1) was described by competitive mechanism with K i equal to 0.15 mM defined from Dixon coordinates. Results of primary screening indicated that substances (2), and (4) acted as competitive inhibitors, while (3) demonstrated characteristics of a non-competitive inhibitor.
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Acknowledgments
The work received financial support from the Russian Foundation for Basic Research (Projects 14-03-31383 mol_a, 13-03-12027 ofi_m) and the Federal Agency for Science and Innovations (Grant of the President of the Russian Federation NSh-21362014.3). The work was also financially supported by Grant PDCPN2013-01 No. 213844 (CONACyT) and SEP-CONACyT Cooperation Program to Promote the Mobility of Researchers. We thank the Mexican Council of Science and Technology (CONACyT) for the financial support under the program “Cátedras-CONACyT” (Researcher No. 2498).
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Maksimov, V., Zaynullin, R., Akhmadiev, N. et al. Inhibitory effect of 4,4′-[ethane-1,2-diylbis(sulfandiylmethanediyl)]bis(3,5-dimethyl-1H-pyrazole) and its derivatives on alpha-amylase activity. Med Chem Res 25, 1384–1389 (2016). https://doi.org/10.1007/s00044-016-1574-2
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DOI: https://doi.org/10.1007/s00044-016-1574-2