Abstract
In a previous paper, we reported that an imidazole derivative 1 exhibited a potent inhibitory activity of 20-HETE synthase (1; IC(50) value of 5.7 nM), but this compound also exhibited little selectivity for cytochrome P450s (CYPs). We examined some derivatives of imidazole 1 which had an amino group on the side chain, and found that a dimethylaminohexyloxy derivative (3g; IC(50) value of 8.8 nM) showed potent and selective inhibitory activity.
MeSH terms
-
Cytochrome P-450 CYP2D6 / metabolism
-
Cytochrome P-450 CYP2D6 Inhibitors
-
Enzyme Inhibitors / chemistry*
-
Enzyme Inhibitors / pharmacology
-
Humans
-
Hydroxyeicosatetraenoic Acids / antagonists & inhibitors*
-
Hydroxyeicosatetraenoic Acids / metabolism
-
Imidazoles / chemistry*
-
Imidazoles / pharmacology
-
Isoenzymes / antagonists & inhibitors
-
Isoenzymes / metabolism
-
Microsomes / drug effects
-
Microsomes / enzymology
Substances
-
Cytochrome P-450 CYP2D6 Inhibitors
-
Enzyme Inhibitors
-
Hydroxyeicosatetraenoic Acids
-
Imidazoles
-
Isoenzymes
-
20-hydroxy-5,8,11,14-eicosatetraenoic acid
-
Cytochrome P-450 CYP2D6