2881-34-7Relevant articles and documents
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels
Gentles, Robert G.,Grant-Young, Katherine,Hu, Shuanghua,Huang, Yazhong,Poss, Michael A.,Andres, Charles,Fiedler, Tracey,Knox, Ronald,Lodge, Nicholas,Weaver, C. David,Harden, David G.
scheme or table, p. 5316 - 5319 (2009/05/07)
An initial SAR study on a series of apamin-displacing 2-aminothiazole KCa2 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.