SYNTHESIS AND ANTIVIRAL ACTIVITY OF NONANNULATED TETRAZOLYLPYRIMIDINES

Authors

  • Владимир А. Островский Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia
  • Геворг Г. Данагулян Russian–Armenian (Slavonic) University, 123 Hovsep Emin St., Yerevan 0051, Armenia Technological Center of Organic and Pharmaceutical Chemistry, National Academy of Sciences of the Republic of Armenia,
  • Ольга М. Нестерова Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia
  • Юлия Н. Павлюкова Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia
  • Владимир В. Толстяков Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia
  • Ольга С. Зарубина Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia
  • Павел А. Слепухин Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 22/20 Sofyi Kovalevskoi St., Yekaterinburg 620108, Russia
  • Яна Л. Есаулкова Saint Petersburg Pasteur Research Institute of Epidemiology and Microbiology, 14 Mira St., Saint Petersburg 197101, Russia
  • Анна А. Мурылева Saint Petersburg Pasteur Research Institute of Epidemiology and Microbiology, 14 Mira St., Saint Petersburg 197101, Russia
  • Владимир В. Зарубаев Saint Petersburg Pasteur Research Institute of Epidemiology and Microbiology, 14 Mira St., Saint Petersburg 197101, Russia
  • Ростислав Е. Трифонов Saint Petersburg State Institute of Technology (Technical University), 26 Moskovsky Ave., Saint Petersburg 190013, Russia

DOI:

https://doi.org/10.1007/6070

Keywords:

pyrimidines, tetrazoles, biological activity, linkers, properties, structure, synthesis.

Abstract

Nonannulated tetrazolylpyrimidines in the structure of which the heterocyclic fragments are separated by hydrazinocarbonylmethyl, methylpyrazolyl groups or a sulfur atom were synthesized. Some of these compounds showed moderate in vitro activity against H1N1 subtype of influenza A virus. The selectivity index of the anti-influenza action of {5-[(4,6-dimethylpyrimidin-2-yl)sulfanyl]-1H-tetrazol-1-yl}acetic acid, which has very low cytotoxicity, was twice as high as the selectivity index of the reference drug rimantadine.

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Published

2021-05-05

Issue

Vol. 57 No. 4 (2021): Heterocycles Against Viruses

Section

Original Papers