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The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

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Pharmaceutical Chemistry Journal Aims and scope

Heating of substituted benzimidazole-2-sulfonic acids in the presence of excess quantities of secondary amines was used to synthesize dialkylaminobenzimidazoles. Experimental studies of potential antiarrhythmic, antiaggregation, hemorheological, AT1 angiotensin- and NHE-1-inhibiting, and antiserotonin activity identified active compounds. 1[-2-(5-Methyl)benzimidazole]pyrrolidine had greater NHE-inhibiting activity than zoniporide. 1-{[2-(5-Methoxy)benzimidazole]-4-N-methyl}piperazine dihydrochloride had greater antiaggregatory activity than acetylsalicylic acid, while 1-[2-(5-methyl)benzimidazole]piperidine was as active as cyproheptadine in terms of 5-HT2A antagonistic activity. 1-(2-Benzimidazole)pyrrolidine and 1-[2-(5-chloro) benzimadazole pyrrolidine dihydrochlorides had 5-HT3 antagonist activity equal to that of tropisetron..

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Authors and Affiliations

  1. Science Research Institute of Physical and Organic Chemistry, Southern Federal University, Rostov-on-Don, Russia

    O. N. Zhukovskaya & V. A. Anisimova

  2. Volgograd State Medical University, Ministry of Health of the Russian Federation, Volgograd, Russia

    A. A. Spasov, D. S. Yakovlev, N. A. Gurova, A. F. Kucheryavenko, O. A. Salaznikova, V. A. Kuznetsova, D. V. Mal’tsev, A. A. Brigadirova, O. A. Solov’eva, V. V. Gurova & E. V. Reznikov

  3. Volgograd Medical Scientific Center, Volgograd, Russia

    A. A. Spasov, D. S. Yakovlev, V. A. Kuznetsova, D. V. Mal’tsev, A. A. Brigadirova & Ya. V. Morkovina

Authors
  1. O. N. Zhukovskaya
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  2. V. A. Anisimova
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  3. A. A. Spasov
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  4. D. S. Yakovlev
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  6. A. F. Kucheryavenko
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  7. O. A. Salaznikova
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  8. V. A. Kuznetsova
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  9. D. V. Mal’tsev
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  10. A. A. Brigadirova
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  11. Ya. V. Morkovina
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  12. O. A. Solov’eva
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  13. V. V. Gurova
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  14. E. V. Reznikov
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Corresponding author

Correspondence to O. N. Zhukovskaya.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 51, No. 3, pp. 20 – 24, March, 2017.

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Zhukovskaya, O.N., Anisimova, V.A., Spasov, A.A. et al. The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles. Pharm Chem J 51, 182–186 (2017). https://doi.org/10.1007/s11094-017-1578-3

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  • DOI: https://doi.org/10.1007/s11094-017-1578-3

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