Computational and Synthetic Target-Based Approaches to the Discovery of Novel Anticonvulsant Compounds

LLANOS, MANUEL AUGUSTO; GAVERNET, LUCIANA; GAROFALO, FEDERICO MARIANO; GANTNER, MELISA EDITH; VILLALBA, MARÍA LUISA

CURRENT MEDICINAL CHEMISTRY.

BENTHAM SCIENCE PUBL LTD

Año: 2021 vol. 28

0929-8673

During the past decades, an important number of anticonvulsant drugs have been incorporated into the collection of drugs to treat epilepsy. However, two main difficulties remain unsolved in therapy: the development of drug-resistant epilepsy and the occurrence of severe toxic effects caused by the medication in responsive patients. The retrospective analysis of the strategies for discovering known anticonvulsant drugs showed that screening campaigns on animal models of epilepsy had been almost the exclusive strategy for identifying the marketed compounds. However, the actual structural and functional information about the molecular targets of the anticonvulsant drugs, and the increasing knowledge of the molecular alterations that generate epileptic seizures, allow a more rational identification of active compounds.