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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

Author(s): Lakshman Saini, S. P. Gupta and V.S.A. Kumar Satuluri

Volume 5 , Issue 6 , 2009

Page: [570 - 576] Pages: 7

DOI: 10.2174/157340609790170524

Price: $65

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


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