Inhibition of mammalian 5-lipoxygenase by 2-benzylaminophenols.
A number of 2-benzylaminophenols, prepared from the corresponding 2-aminophenols by reductive alkylation, have been identified as highly potent inhibitors of 5-lipoxygenase with IC50 values in the nanomolar range. Most compounds were also shown to inhibit the release of the peptidoleukotrienes when administered intraperitoneally in a rat model of peritoneal anaphylaxis. Two compounds evaluated for their effects on anaphylactic contractions in isolated human lung were shown to attenuate the leukotriene-induced component of the response.
Buckle
D R
DR
Beecham Pharmaceuticals, Research Division, Biosciences Research Centre, Epsom, Surrey, UK.
Bumstead
J
J
Clarke
G D
GD
Foster
K A
KA
Parr
H
H
Taylor
J F
JF
Thody
V E
VE
Webster
R A
RA
D000627:Aminophenols / Q000494:pharmacology*; D000707:Anaphylaxis; D000818:Animals; D001091:Arachidonate Lipoxygenases / Q000037:antagonists & inhibitors*; D006801:Humans; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors; D008168:Lung / Q000187:drug effects; D008832:Microchemistry; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D013189:SRS-A / Q000378:metabolism
D000627:Aminophenols; D016859:Lipoxygenase Inhibitors; D013189:SRS-A; D001091:Arachidonate Lipoxygenases