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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

A method of preparing the potential analgesic substance 4,10-bis((±)-5-benzoyl-2,3-dihydro-1 H -pyrrolo-[1,2- a ]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0 3,11 ,0 5,9 ]dodecane is described in detail. Different conditions for preparing the target substance are co...

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Published in:Pharmaceutical chemistry journal 2021-02, Vol.54 (11), p.1140-1144
Main Authors: Kulagina, D. A., Sysolyatin, S. V., Kalashnikov, A. I., Malykhin, V. V., Sonina, E. G., Shevchenko, A. V., Krylova, S. G., Lopatina, K. A., Zueva, E. P., Razina, T. G., Rybalkina, O. Yu, Amosova, E. N.
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Language:English
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Summary:A method of preparing the potential analgesic substance 4,10-bis((±)-5-benzoyl-2,3-dihydro-1 H -pyrrolo-[1,2- a ]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0 3,11 ,0 5,9 ]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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-021-02332-0