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Weaver Lab

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

AUTHORS

Gentles RGRobert G , Grant-Young K Katherine , Hu S Shuanghua , Huang Y Yazhong , Poss MA Michael A , Andres C Charles , Fiedler T Tracey , Knox R Ronald , Lodge N Nicholas , Weaver CD C David , Harden DG David G . Bioorganic & medicinal chemistry letters. 2008 10 1; 18(19). 5316-9

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.

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.