Cyclocondensation of α-halogenacetophenones with an original 4-morpholine thiosemicarbazide was used to synthesize a group of new Captions: of the 1,3,4-thiadiazine group, containing a thiomorpholine fragment at position 2 of the thiadiazine ring. Two members of this group of compounds were found to produce effective inhibition of nonenzymatic protein glycosylation in an in vitro model system. These test results allow compounds containing phenyl and fluorophenyl fragments IIIa and IIIb to be recommended for further study in in vivo experiments.
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References
US Patent 6 028 068, Chem. Abstr., 127, 149163 (1997).
Russian Federation Patent 2411936, Chem. Abstr., 154, 251130 (2011).
PCT Rus. Patent 2259371, Chem. Abstr., 143, 229887 (2005).
A. Sarapultsev, O. Chupakhin, M. Rantsev, et al., Adv. Biosci. Biotechnol., 3, 442 – 448 (2012).
P. Sarapultsev, O. Chupakhin, A. Sarapultsev, et al., Int. J. Exp. Pathol., 93(1), 18 – 23 (2012).
L. P. Sidorova, N. M. Perova, L. G. Egorova, A. P. Novikova, Proceedings of the First All-Union Conference on Theoretical Organic Chemistry [in Russian], Volgograd (1991), p. 232.
O. N. Chupakhin, L. P. Sidorova, N. M. Perova, et al., Collection of Reports from the Fourth International Conference SVS-2010, “The Chemistry and Biological Activity of Synthetic and Natural Compounds”, [in Russian], ICSPF Inter Bio Screen Ltd., Moscow (2010), cs. 489.
L. P. Sidorova, T. A. Tseitler, N. M. Perova, et al., Khim-Farm. Zh., 49(8), 8 – 12 (2015); Pharm. Chem. J., 49(8), 501 – 505 (2015).
V. V. Emel’yanov, E. A. Savateeva, L. P. Sidorova, et al., RIZh, 9, 2(1), (18), 487 – 489 (2015).
US Patent, Chem. Abstr., 127, 149164 (1997).
V. V. Emel’yanov, E. A. Savateeva, A. V. Musal’nikova, et al., Allergol. Immunol., 14(2), 141 – 142 (2013).
I. Sadowska-Bartosz, S. Galiniak, G. Bartosz, Molecules, 19, 18828 – 18849 (2014).
L. N. Viktorova, V. K. Gorodetskii, Lab. Delo, 5, 15–18 (1990).
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 51, No. 1, pp. 11 – 14, January, 2017.
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Sidorova, L.P., Tseitler, T.A., Emel’yanov, V.V. et al. 2-Thiomorpholino-5-Aryl-6H-1,3,4-Thiadiazine Hydrobromides and Their Ability to Inhibit Nonenzymatic Protein Glycosylation. Pharm Chem J 51, 9–12 (2017). https://doi.org/10.1007/s11094-017-1547-x
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DOI: https://doi.org/10.1007/s11094-017-1547-x