Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton

…, E Russo, G De Sarro, A Chimirri

Index: Gitto, Rosaria; Barreca, Maria Letizia; De Luca, Laura; De Sarro, Giovambattista; Ferreri, Guido; Quartarone, Silvana; Russo, Emilio; Constanti, Andrew; Chimirri, Alba Journal of Medicinal Chemistry, 2003 , vol. 46, # 1 p. 197 - 200

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Citation Number: 34

Abstract

In our studies on the development of new anticonvulsants, we planned the synthesis of N- substituted 1, 2, 3, 4-tetrahydroisoquinolines to explore the structure-activity relationships. All derivatives were evaluated against audiogenic seizures in DBA/2 mice, and the 1-(4'- bromophenyl)-6, 7-dimethoxy-2-(piperidin-1-ylacetyl) derivative (26) showed the highest activity with a potency comparable to that of talampanel, the only noncompetitive α-amino- ...