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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

Sodium Channel Blocking Activity and In-vivo Testing of New Phenylimidazole Derivatives

Author(s): Mirko Rivara, Manoj K. Patel, Alberto Rapalli and Valentina Zuliani

Volume 13, Issue 9, 2016

Page: [962 - 967] Pages: 6

DOI: 10.2174/1570180813666160714125755

Price: $65

Abstract

We previously reported the discovery of diphenylimidazoles as potent sodium channel blockers, potentially useful in the treatment of epilepsy. In this work we further explore the structural requirements necessary for the potency of these derivatives with the aim to understand which structural modifications of the original scaffold could be tolerated in order to retain activity. We have synthesized new compounds working on the 2-position of the imidazole ring. First we have introduced a carbonyl spacer, that was subsequently reduced to alcohol. Both carbonyl and alcohol derivatives have been tested for their ability to block NaV1.6 sodium channel subtype in vitro and for their antiepileptic activity in rodent acute seizures models.

Keywords: Sodium channels, patch clamp electrophysiology, NaV1.6, Phenyl-imidazoles.

Graphical Abstract


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