Synthesis and structure active relationship of 1 aryl 6,7 dimethoxy 1,2,3,4 tetrahydroisoquinoline anticonvulsants.

Publication: Chemical & pharmaceutical bulletin
Publication Date: 2010
Study Author(s): Gitto, Rosaria;De Luca, Laura;Ferro, Stefania;Agnello, Stefano;Russo, Emilio;De Sarro, Giovanbattista;Chimirri, Alba;
Institution: Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
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We have previously disclosed that some 6,7-dimethoxyisoquinoline derivatives are able to produce anticonvulsant effects in different animal models of Epilepsy. Following these studies this paper describes the synthesis of a small series of new 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines strictly related to previously reported analogues. This novel series of isoquinolines was designed on the basis of well defined structure-active relationship (SAR) information already acquired for this class of anticonvulsant agents. The pharmacological effects of the new synthesized compounds were evaluated against audiogenic Seizures in Dilute Brown non-Agouti (DBA/2) mice. The preliminary pharmacological screening led to the identification of a new active molecule the 2-acetyl-1-(4'-methylphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (6d) that displayed significant anticonvulsant activity. Computational studies helped to rationalize these obtained pharmacological results.
PMID: 21139262

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