Substituted biaryl pyrazoles as sodium channel blockers

descriptionPublicationkeyboard_double_arrow_right Article 01 Sep 2010 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 20, pages 5,480-5,483 (issn: 0960-894X,

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Authors: Sriram, Tyagarajan; Prasun K, Chakravarty; Bishan, Zhou; Brett, Taylor; Michael H, Fisher; Mathew J, Wyvratt; Kathy, Lyons; +16 Authors

doi: 10.1016/j.bmcl.2010.07.080

pmid: 20709545

Substituted biaryl pyrazoles as sodium channel blockers

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Abstract

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 Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain.

Related Organizations

Merck & Co.
United States

Keywords

NAV1.7 Voltage-Gated Sodium Channel, Haplorhini, Sodium Channels, Rats, Structure-Activity Relationship, Dogs, Microsomes, Liver, Animals, Humans, Neuralgia, Pyrazoles, Sodium Channel Blockers

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