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Synthesis and Analgesic Activity of 4,10-Bis((±)-5-Benzoyl-2,3-Dihydro-1hpyrrolo[1,2-a]Pyrrole-1-Carbonyl)-2,6,8,12-Tetraacetyl-2,4,6,8,10,12-Hexaazatetracyclo[5,5,03,11,05,9]Dodecane

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Pharmaceutical Chemistry Journal Aims and scope

A method of preparing the potential analgesic substance 4,10-bis((±)-5-benzoyl-2,3-dihydro-1H-pyrrolo-[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,03,11,05,9]dodecane is described in detail. Different conditions for preparing the target substance are considered and its full physicochemical properties are presented. Marked analgesic activity of this innovatory compound was found in conditions of thermal nociception in the hotplate test and acute visceral and somatic deep pain in the acetic writhings test.

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Authors and Affiliations

  1. Institute of Problems in Chemical and Energy Technology, Siberian Branch, Russian Academy of Sciences, 1, Sotsialisticheskaya Street, 659322, Biysk, Russia

    D. A. Kulagina, S. V. Sysolyatin, A. I. Kalashnikov, V. V. Malykhin, E. G. Sonina & A. V. Shevchenko

  2. E. D. Goldberg Science Research Institute of Pharmacology and Regenerative Medicine, Tomsk National Medical Research Center, Russian Academy of Sciences, 3 Lenin Prospekt, 634028, Tomsk, Russia

    S. G. Krylova, K. A. Lopatina, E. P. Zueva, T. G. Razina, O. Yu. Rybalkina & E. N. Amosova

Authors
  1. D. A. Kulagina
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  2. S. V. Sysolyatin
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  3. A. I. Kalashnikov
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  4. V. V. Malykhin
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  5. E. G. Sonina
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  6. A. V. Shevchenko
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  7. S. G. Krylova
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  8. K. A. Lopatina
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  9. E. P. Zueva
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  10. T. G. Razina
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  11. O. Yu. Rybalkina
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  12. E. N. Amosova
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Corresponding author

Correspondence to E. N. Amosova.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 11, pp. 35 – 39, November, 2020.

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Kulagina, D.A., Sysolyatin, S.V., Kalashnikov, A.I. et al. Synthesis and Analgesic Activity of 4,10-Bis((±)-5-Benzoyl-2,3-Dihydro-1hpyrrolo[1,2-a]Pyrrole-1-Carbonyl)-2,6,8,12-Tetraacetyl-2,4,6,8,10,12-Hexaazatetracyclo[5,5,03,11,05,9]Dodecane. Pharm Chem J 54, 1140–1144 (2021). https://doi.org/10.1007/s11094-021-02332-0

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  • DOI: https://doi.org/10.1007/s11094-021-02332-0

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