The publication presents a number of modifications based on electrophilic reactions of previously synthesized biologically active benzannulated pyrrolo[1,2-a]imidazolones and pyrrolo[2,1-b]quinazolinones, which make it possible to widely change the physicochemical properties of molecules. Quantitative assessments of the lipophilicity of all synthesized compounds were carried out, on the basis of which conclusions were made regarding the advisability of introducing alkyl and trifluoroacetyl groups to increase the bioavailability of compounds by increasing their lipophilicity to 40%.
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The study was supported by a grant of the Russian Science Foundation (project No. 19-73-00218).
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, 2020, 56(7), 923–929
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Grinev, V.S., Egorova, A.Y. Electrophilic reactions as methods of modification of pyrrolobenzimidazolones and pyrroloquinazolinones. Chem Heterocycl Comp 56, 923–929 (2020). https://doi.org/10.1007/s10593-020-02751-z
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DOI: https://doi.org/10.1007/s10593-020-02751-z