TOPIC

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

Journal

Bioorganic & Medicinal Chemistry Letters

Author(s)

Mark J.Wall, Nalin L.Subasinghe, Michael P.Winters. Mary Lou Lubin, Michael F.A. Finley, Ning Qin Michael, R. Brandt, Michael P.Neeper, Craig R. Schneider, Raymond W.Colburn, Christopher M. Flores, Zhihua Sui

Year

2018

A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.

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