66040-39-9Relevant articles and documents
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
experimental part, p. 1602 - 1605 (2011/02/22)
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.
Development of the Pictet-Spengler reaction catalyzed by AuCl 3/AgOTf
Youn, So Won
, p. 2521 - 2523 (2007/10/03)
Mild and efficient AuCl3/AgOTf-catalyzed Pictet-Spengler reactions were developed to afford in good yields a variety of tetrahydroisoquinoline and tetrahydro-β-carboline ring systems, which constitute important motifs in biologically active nat
