Inhibition of Na V 1.6 sodium channel currents by a novel series of 1, 4-disubstituted-triazole derivatives obtained via copper-catalyzed click chemistry

M Rivara, MK Patel, L Amori, V Zuliani

Index: Rivara, Mirko; Patel, Manoj K.; Amori, Laura; Zuliani, Valentina Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 20 p. 6401 - 6404

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Citation Number: 10

Abstract

We have synthesized and evaluated a series of 1, 4-disubstituted-triazole derivatives for inhibition of the rat NaV1. 6 sodium channel isoform, an isoform thought to play an important role in controlling neuronal firing. Starting from a series of 2, 4 (1H)-diarylimidazoles previously published, we decided to extend the SAR study by replacing the imidazole with a different heterocyclic scaffold and by varying the aryl substituents on the central aromatic ...