Title: A QSAR Study on Some Series of Sodium and Potassium Channel Blockers
Volume: 5
Issue: 6
Author(s): Lakshman Saini, S. P. Gupta and V.S.A. Kumar Satuluri
Affiliation:
Keywords:
QSAR study, sodium channel blockers, potassium channel blockers, pyrazoles, arylimidazoles, khellinone derivatives
Abstract: 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.
