In our previous studies a ligand-based approach led to the identification of noncompetitive AMPA receptor antagonists containing isoquinoline scaffold. In an attempt to perform a systematic SAR study, we synthesized new N-substituted-isoquinolines bearing the most salient features described by our 3D pharmacophore model. All compounds were screened against audiogenic seizures and some derivatives showed anticonvulsant properties. Compound 24, the most active of the series, was also tested in vitro using the patch-clamp technique and proved to antagonize AMPA-mediated effects. (C) 2007 Elsevier Ltd. All rights reserved.
Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists
CITRARO R;DE SARRO G;
2008-01-01
Abstract
In our previous studies a ligand-based approach led to the identification of noncompetitive AMPA receptor antagonists containing isoquinoline scaffold. In an attempt to perform a systematic SAR study, we synthesized new N-substituted-isoquinolines bearing the most salient features described by our 3D pharmacophore model. All compounds were screened against audiogenic seizures and some derivatives showed anticonvulsant properties. Compound 24, the most active of the series, was also tested in vitro using the patch-clamp technique and proved to antagonize AMPA-mediated effects. (C) 2007 Elsevier Ltd. All rights reserved.File in questo prodotto:
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