Lakshman Saini, S. P. Gupta and V.S.A. Kumar Satuluri Pages 570 - 576 ( 7 )
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.
QSAR study, sodium channel blockers, potassium channel blockers, pyrazoles, arylimidazoles, khellinone derivatives
Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut-250005, India.