The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

O. N. Zhukovskaya; 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

doi:10.1007/s11094-017-1578-3

The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

Authors: Zhukovskaya O.N.¹, Anisimova V.A.¹, Spasov A.A.²^,3, Yakovlev D.S.²^,3, Gurova N.A.², Kucheryavenko A.F.², Salaznikova O.A.², Kuznetsova V.A.²^,3, Mal’tsev D.V.²^,3, Brigadirova A.A.²^,3, Morkovina Y.V.³, Solov’eva O.A.², Gurova V.V.², Reznikov E.V.²
Affiliations:
1. Science Research Institute of Physical and Organic Chemistry, Southern Federal University
2. Volgograd State Medical University, Ministry of Health of the Russian Federation
3. Volgograd Medical Scientific Center
Issue: Vol 51, No 3 (2017)
Pages: 182-186
Section: Article
URL: https://journals.rcsi.science/0091-150X/article/view/244525
DOI: https://doi.org/10.1007/s11094-017-1578-3
ID: 244525

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Abstract

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-HT_2A 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-HT_2A receptor blockers, 5-HT₃ receptor blockers, angiotensin 1 receptor blockers

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The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

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Abstract

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About the authors

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