4.5 Article

Substituted biaryl pyrazoles as sodium channel blockers

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 18, 页码 5480-5483

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.080

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Neuropathic pain; Voltage gated sodium channel; Na(v)1.7 blockers; Biaryl pyrazoles; Chung model

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Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Na(v)1.7 blocker has excellent efficacy in the Chung model of neuropathic pain. (c) 2010 Elsevier Ltd. All rights reserved.

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