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Pharmaceutical Chemistry Journal

, Volume 51, Issue 3, pp 182–186 | Cite as

The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

  • O. N. ZhukovskayaEmail author
  • V. A. Anisimova
  • 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
  • Ya. V. Morkovina
  • O. A. Solov’eva
  • V. V. Gurova
  • E. V. Reznikov
Article

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..

Keywords

dialkylaminobenzimidazoles synthesis antiarrhythmic antiaggregatory hemorheological NHE-inhibiting activity 5-HT2A receptor blockers 5-HT3 receptor blockers angiotensin 1 receptor blockers 

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Copyright information

© Springer Science+Business Media, LLC 2017

Authors and Affiliations

  • O. N. Zhukovskaya
    • 1
    Email author
  • V. A. Anisimova
    • 1
  • A. A. Spasov
    • 2
    • 3
  • D. S. Yakovlev
    • 2
    • 3
  • N. A. Gurova
    • 2
  • A. F. Kucheryavenko
    • 2
  • O. A. Salaznikova
    • 2
  • V. A. Kuznetsova
    • 2
    • 3
  • D. V. Mal’tsev
    • 2
    • 3
  • A. A. Brigadirova
    • 2
    • 3
  • Ya. V. Morkovina
    • 3
  • O. A. Solov’eva
    • 2
  • V. V. Gurova
    • 2
  • E. V. Reznikov
    • 2
  1. 1.Science Research Institute of Physical and Organic ChemistrySouthern Federal UniversityRostov-on-DonRussia
  2. 2.Volgograd State Medical University, Ministry of Health of the Russian FederationVolgogradRussia
  3. 3.Volgograd Medical Scientific CenterVolgogradRussia

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