A QSAR study on some series of sodium and potassium channel blockers

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.