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

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.