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.
MeSH terms
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Apamin / pharmacology*
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Combinatorial Chemistry Techniques
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Molecular Structure
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Potassium Channel Blockers / chemical synthesis*
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Potassium Channel Blockers / chemistry
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Potassium Channel Blockers / pharmacology*
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology*
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Small-Conductance Calcium-Activated Potassium Channels / antagonists & inhibitors*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology*
Substances
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N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine
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Potassium Channel Blockers
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Pyridines
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Small-Conductance Calcium-Activated Potassium Channels
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Thiazoles
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Apamin