1282448-43-4Relevant academic research and scientific papers
Synthesis and structure - Active relationship of 1-aryl-6,7-dimethoxy-1,2, 3,4-tetrahydroisoquinoline anticonvulsants
Gitto, Rosaria,De Luca, Laura,Ferro, Stefania,Agnello, Stefano,Russo, Emilio,De Sarro, Giovanbattista,Chimirri, Alba
, p. 1602 - 1605 (2010)
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.
