2. Academic Validation
  3. Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels

Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5316-9. doi: 10.1016/j.bmcl.2008.08.023.
Robert G Gentles 1,  Katherine Grant-Young,  Shuanghua Hu,  Yazhong Huang,  Michael A Poss,  Charles Andres,  Tracey Fiedler,  Ronald Knox,  Nicholas Lodge,  C David Weaver,  David G Harden
Affiliations

Affiliation

  • 1 Research and Development, Bristol Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA. robert.gentles@bms.com
PMID: 18774291 DOI: 10.1016/j.bmcl.2008.08.023
Abstract

An initial SAR study on a series of apamin-displacing 2-aminothiazole K(CA)2 channel blockers is described. Potent inhibitors such as N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (13) are disclosed, and for select members of the series, the relationship between the observed activity in a thallium flux, a binding and a whole-cell electrophysiology assay is presented.

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