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.
Keywords: QSAR study, sodium channel blockers, potassium channel blockers, pyrazoles, arylimidazoles, khellinone derivatives
Medicinal Chemistry
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.
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Cite this article as:
Saini Lakshman, Gupta P. S. and Satuluri Kumar V.S.A., A QSAR Study on Some Series of Sodium and Potassium Channel Blockers, Medicinal Chemistry 2009; 5 (6) . https://dx.doi.org/10.2174/157340609790170524
DOI https://dx.doi.org/10.2174/157340609790170524 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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