Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators.

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ID: 77180
2019
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Ranked #25 of 246 articles by views in Bioorganic & medicinal chemistry letters

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Abstract
Effective treatments of neuropathic pain have been a focus of many discovery programs. KCNQ (kv7) are voltage gated potassium channel openers that have the potential for the treatment of CNS disorders including neuropathic pain. Clinical studies have suggested agents such as Retigabine to be a modulator of pain-like effects such as hyperalgesia and allodynia. In this paper, we describe the discovery and evaluation of a series of novel pyrazolopyrimidines and their affinity for potassium channels KCNQ2/3. These pyrazolopyrimidines have also shown good efficacy in the capsaicin-induced acute and secondary mechanical allodynia model and excellent pharmacokinetic properties, which may be superior to Retigabine.
Reference Key
osuma2019designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Osuma, Augustine T;Xu, Xiangdong;Wang, Zhi;Van Camp, Jennifer A;Freiberg, Gail M;
Journal Bioorganic & medicinal chemistry letters
Year 2019
DOI
S0960-894X(19)30533-5
URL
Keywords
potassium channel kcnq kv7

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