Skip to main content
Log in

2-Thiomorpholino-5-Aryl-6H-1,3,4-Thiadiazine Hydrobromides and Their Ability to Inhibit Nonenzymatic Protein Glycosylation

  • SEARCH FOR NEW DRUGS
  • Published:
Pharmaceutical Chemistry Journal Aims and scope

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Scheme 1.
Scheme 2.
Fig. 1.

Similar content being viewed by others

References

  1. US Patent 6 028 068, Chem. Abstr., 127, 149163 (1997).

  2. Russian Federation Patent 2411936, Chem. Abstr., 154, 251130 (2011).

  3. PCT Rus. Patent 2259371, Chem. Abstr., 143, 229887 (2005).

  4. A. Sarapultsev, O. Chupakhin, M. Rantsev, et al., Adv. Biosci. Biotechnol., 3, 442 – 448 (2012).

    Article  Google Scholar 

  5. P. Sarapultsev, O. Chupakhin, A. Sarapultsev, et al., Int. J. Exp. Pathol., 93(1), 18 – 23 (2012).

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  6. 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.

  7. 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.

  8. 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).

  9. V. V. Emel’yanov, E. A. Savateeva, L. P. Sidorova, et al., RIZh, 9, 2(1), (18), 487 – 489 (2015).

  10. US Patent, Chem. Abstr., 127, 149164 (1997).

  11. V. V. Emel’yanov, E. A. Savateeva, A. V. Musal’nikova, et al., Allergol. Immunol., 14(2), 141 – 142 (2013).

    Google Scholar 

  12. I. Sadowska-Bartosz, S. Galiniak, G. Bartosz, Molecules, 19, 18828 – 18849 (2014).

    Article  PubMed  Google Scholar 

  13. L. N. Viktorova, V. K. Gorodetskii, Lab. Delo, 5, 15–18 (1990).

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to L. P. Sidorova.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 51, No. 1, pp. 11 – 14, January, 2017.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

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

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11094-017-1547-x

Keywords

Navigation