SYNTHESIS OF HYDROGENATED 2,7-DIMETHYLPYRROLO[3,4-<i>b</i>]INDOLES – ANALOGS OF DIMEBON

Abstract

A schemes have been proposed for the synthesis of novel 4-substituted 2,7-dimethyl-3,4-dihydro-1H- and previously unknown 2,7-dimethyl-cis-1,2,3,3a,4,8b-hexahydropyrrolo[3,4-b]indoles. In the case of the Dimebon structural analog 2,7-dimethyl-4-[2-(6-methylpyridin-3-yl)ethyl]-3,4-dihydro-1H-pyrrolo[3,4-b]indole a broad spectrum of pharmacological activity was found in the hydrogenated pyrroloindoles suitable for the development of medicines via the "magic bullet" concept. A strong dependence of the antagonist relationship of the synthesized compounds towards histamine H₁ and serotonin 5-HT₆ receptors with the nature of the substituent in the 4 position and the degree of hydrogenation of the pyrrolo[3,4-b]indoles was demonstrated.

How to Cite
Ivachtchenko, A. V.; Frolov, E. B.; Mitkin, O. D.; Tkachenko, S. E.; Khvat, A. V. Chem. Heterocycl. Compd. 2010, 46, 170. [Khim. Geterotsikl. Soedin. 2010, 209.]

For this article in the English edition see DOI 10.1007/s10593-010-0488-z