The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles

作者：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

来源：Pharmaceutical Chemistry Journal, 2017, 51(3): 182-186.

DOI：10.1007/s11094-017-1578-3

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

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-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.

• 出版日期2017-6