[Lipoxygenase inhibitors. IV. Synthesis and cyclization reactions of open-chain N1-aryl-substituted amidrazones].
alpha-Carbonyl carboxylic acid arylhydrazonochlorides obtained by Japp-Klingemann reaction are the starting substances for the synthesis of alpha-carbonyl carboxylic acid arylhydrazonoamides, -esters and -thioesters. The inhibiting activity of these compounds against 15- and 5-lipoxygenase is described. Reactions of derivatives of amidrazones with formaldehyde give triazole, triazoline and unexpected benzotriazepine derivatives.
Frohberg
P
P
Institut für Phamrazeutische Chemie der Martin-Luther-Universität Halle-Wittenberg, Halle.
Kupfer
C
C
Stenger
P
P
Baumeister
U
U
Nuhn
P
P
D000818:Animals; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D051379:Mice; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology
D006835:Hydrazones; D016859:Lipoxygenase Inhibitors; D007975:Leukotriene B4
Lipoxygenase-Inhibitoren, 4.Mitt.1): Synthese und Cyclisierungsreaktionen offenkettiger N1-arylsubstituierter Amidrazone.