Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.

doi:10.1021/acs.jmedchem.9b00796

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Article

Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.

Journal of medicinal chemistry - 9 Jan 2020

Ostacolo Carmine, Miceli Francesco, Di Sarno Veronica, Nappi Piera, Iraci Nunzio, Soldovieri Maria Virginia, Ciaglia Tania, Ambrosino Paolo, Vestuto Vincenzo, Lauritano Anna, Musella Simona, Pepe Giacomo, Basilicata Manuela Giovanna, Manfra Michele, Perinelli Diego Romano, Novellino Ettore, Bertamino Alessia, Gomez-Monterrey Isabel M, Campiglia Pietro, Taglialatela Maurizio

Abstract excerpt

Kv7 K+ channels represent attractive pharmacological targets for the treatment of different neurological disorders, including epilepsy. In this paper, 42 conformationally restricted analogues of the prototypical Kv7 activator retigabine have been synthesized and tested by electrophysiological patch-clamp experiments as Kv7 agonists. When compared to retigabine (0.93 ± 0.43 μM), the EC50s for Kv7.2 current...

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PMID: 31815462
DOI: 10.1021/acs.jmedchem.9b00796

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