title: Inhibition of mammalian 5-lipoxygenase by 2-benzylaminophenols.
abstract: 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.
authors.affiliation: Beecham Pharmaceuticals, Research Division, Biosciences Research Centre, Epsom, Surrey, UK.
authors.forename: D R
authors.initials: DR
authors.lastname: Buckle
authors.forename: J
authors.initials: J
authors.lastname: Bumstead
authors.forename: G D
authors.initials: GD
authors.lastname: Clarke
authors.forename: K A
authors.initials: KA
authors.lastname: Foster
authors.forename: H
authors.initials: H
authors.lastname: Parr
authors.forename: J F
authors.initials: JF
authors.lastname: Taylor
authors.forename: V E
authors.initials: VE
authors.lastname: Thody
authors.forename: R A
authors.initials: RA
authors.lastname: Webster
mesh_terms: 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
chemical_list: D000627:Aminophenols; D016859:Lipoxygenase Inhibitors; D013189:SRS-A; D001091:Arachidonate Lipoxygenases