The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

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, AT 1 angiotensin- and NHE-1-inhibiting, and antiseroto...

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Published in:Pharmaceutical chemistry journal 2017-06, Vol.51 (3), p.182-186
Main Authors: Zhukovskaya, O. N., Anisimova, V. A., Spasov, A. A., Yakovlev, D. S., Gurova, N. A., Kucheryavenko, A. F., Salaznikova, O. A., Kuznetsova, V. A., Mal’tsev, D. V., Brigadirova, A. A., Morkovina, Ya. V., Solov’eva, O. A., Gurova, V. V., Reznikov, E. V.
Format: Article
Language:English
Subjects:
Antiarrhythmia agents
Aspirin
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Sulfonic acids
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Summary: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, AT 1 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-HT 3 antagonist activity equal to that of tropisetron..
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-017-1578-3