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
- PMID: 18774291[PubMed].
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.