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A QSAR Study on Some Series of Sodium and Potassium Channel Blockers

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A quantitative-structure activity relationship (QSAR) study has been made on two different series of sodium channel blockers – namely, a series of 3-(4-phenoxyphenyl)pyrazoles and a series of 2-alkyl-4-arylimidazoles – and a series of potassium channel blockers that comprises of khellinone derivatives, which act on voltage-gated K+ channels Kv1.3. In both the cases – the inhibition of Na+ channels or the inhibition of K+ channels – the significant correlations were obtained between the inhibition potencies and the hydrophobic properties of the compounds. This led to suggest that the hydrophobic property of the compounds is a major determining factor of the Na+/ K+ channel blocking activity and that the compounds might elicit their effects through the hydrophobic interactions with the receptors.

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Keywords: QSAR study; arylimidazoles; khellinone derivatives; potassium channel blockers; pyrazoles; sodium channel blockers

Document Type: Research Article

Publication date: November 1, 2009

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