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, 20 (22), 6812-5

Subtype-selective Na(v)1.8 Sodium Channel Blockers: Identification of Potent, Orally Active Nicotinamide Derivatives

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Subtype-selective Na(v)1.8 Sodium Channel Blockers: Identification of Potent, Orally Active Nicotinamide Derivatives

Michael E Kort et al. Bioorg Med Chem Lett.

Abstract

A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain.

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