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.
Saini
Lakshman
L
Department of Pharmaceutical Technology, Meerut institute of Engineering and Technology, Meerut-250005, India.
Gupta
S P
SP
Kumar Satluri
V S A
VS
D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D026902:Potassium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship; D012044:Regression Analysis; D026941:Sodium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D001572:Benzofurans; D007093:Imidazoles; D026902:Potassium Channel Blockers; D011720:Pyrazoles; D026941:Sodium Channel Blockers; C509273:khellinone