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Synthesis, Analysis, and Acute Toxicity of 9-(2-diethylaminoethyl)-2-phenylimidazo[1,2-α]benzimidazole Dinitrate

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The key synthetic stage (cyclization) of 9-(2-diethylaminoethyl)-2-phenylimidazo[1,2-α]benzimidazole dinitrate, which possesses antiulcer activity, was improved by changing the reaction medium and using the imine itself rather than its hydrobromide for the cyclization. A method using the physicochemical properties (NMR and IR spectroscopy and UV spectrophotometry) of the substance was proposed for identifying it. An HPLC method was proposed for determining related impurities; nonaqueous titration, for quantitative determination. Acute toxicity was studied in mice and rats upon intragastric and intravenous administration. The results showed that the drug substance had class 3 moderate toxicity upon both intragastric and intravenous administration.

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Acknowledgments

The chemical part of the article was prepared by Southern Federal University with financial support from the Ministry of Science and Higher Education of the Russian Federation [State Task for Scientific Activity, Southern Federal University, 2020, Project FENW-2020-0031 (0852-2020-0031)].

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Authors and Affiliations

  1. Pyatigorsk Medico-Pharmaceutical Institute, Branch of Volgograd State Medical University, 11 Kalinina Prosp., Pyatigorsk, 357532, Russia

    D. O. Mitrakova, M. V. Chernikov & I. P. Remezova

  2. Volgograd State Medical University, 1 Pavshikh Bortsov Sq., Volgograd, 400131, Russia

    A. A. Spasov

  3. Institute of Physical and Organic Chemistry, Southern Federal University, 194/2 Stachki Prosp., Rostov-on-Don, 344090, Russia

    A. S. Morkovnik, L. N. Divaeva & O. N. Zhukovskaya

  4. State Scientific Center for Expertise of Medical Products, Ministry of Health of the Russian Federation, 8 Petrovskii Blvd., Moscow, 127051, Russia

    N. D. Bunyatyan

  5. Sechenov First Moscow State Medical University (Sechenov University), 8/2 Trubetskaya St., Moscow, 119991, Russia

    N. D. Bunyatyan

  6. State Institute of Drugs and Good Medical Practices, 6 Lavrov Per., Moscow, 109044, Russia

    A. V. Morosov

Authors
  1. D. O. Mitrakova
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  2. M. V. Chernikov
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  3. A. A. Spasov
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  4. A. S. Morkovnik
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  5. I. P. Remezova
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  6. N. D. Bunyatyan
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  7. A. V. Morosov
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  8. L. N. Divaeva
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  9. O. N. Zhukovskaya
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Corresponding author

Correspondence to D. O. Mitrakova.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 6, pp. 16 – 22, June, 2021.

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Mitrakova, D.O., Chernikov, M.V., Spasov, A.A. et al. Synthesis, Analysis, and Acute Toxicity of 9-(2-diethylaminoethyl)-2-phenylimidazo[1,2-α]benzimidazole Dinitrate. Pharm Chem J 55, 544–550 (2021). https://doi.org/10.1007/s11094-021-02457-2

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  • DOI: https://doi.org/10.1007/s11094-021-02457-2

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