Artículo

Several New Diverse Anticonvulsant Agents Discovered in a Virtual Screening Campaign Aimed at Novel Antiepileptic Drugs to Treat Refractory Epilepsy

Di Ianni, Mauricio Emiliano Icon; Enrique, Andrea Verónica Icon; Palestro, Pablo Hernán Icon; Gavernet, Luciana Icon; Talevi, Alan Icon; Bruno Blanch, Luis Enrique

Otros responsables

Fecha

12/2012

Editorial

American Chemical Society

Revista

Journal of Chemical Information and Modeling

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Institución organizadora

ISSN

1549-9596

eISSN

ISBN

Idioma

Inglés

Tipo del evento

Clasificación temática

Resumen

A virtual screening campaign was conducted in order to discover new anticonvulsant drug candidates for the treatment of refractory epilepsy. To this purpose, a topological discriminant function to identify antiMES drugs and a sequential filtering methodology to discriminate P-glycopro- tein substrates and nonsubstrates were jointly applied to ZINC 5 and DrugBank databases. The virtual filters combine an ensemble of 2D classifiers and docking simulations. In the light of the results, 10 structurally diverse compounds were acquired and tested in animal models of seizure and the rotorod test. All 10 candidates showed some level of protection against MES test.

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