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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.
Affiliation
  • Gentles RG; Research and Development, Bristol Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492, USA. robert.gentles@bms.com
Bioorg Med Chem Lett ; 18(19): 5316-9, 2008 Oct 01.
Article in En | MEDLINE | ID: mdl-18774291
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Apamin / Pyridines / Thiazoles / Potassium Channel Blockers / Small-Conductance Calcium-Activated Potassium Channels Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Document type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Apamin / Pyridines / Thiazoles / Potassium Channel Blockers / Small-Conductance Calcium-Activated Potassium Channels Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2008 Document type: Article Affiliation country: United States