Anthralin derivatives--inhibition of 5-lipoxygenase--antipsoriatic efficacy.
Inhibition of 5-lipoxygenase by anthralin (1) and 41 derivatives is determined: the acids 38 and 39, the lactones 40-42 and 9-anthrone (8) are the most potent inhibitors, the lactone 41 reaching the efficacy of nordihydroguaiaretic acid (NDGA). The results were correlated with the hydrophilic/lipophilic balance of the test compounds and their clinical efficacy as far as known. There is no correlation between the "minimum structure" of Krebs and Schaltegger concerning antipsoriatic activity and the inhibitory effects against 5-lipoxygenase.
Tanzer
H
H
Institute of Pharmacy, University, Regensburg, Germany.
Braun
C
C
Seidel
M
M
Wiegrebe
W
W
D000818:Animals; D000875:Anthralin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D002417:Cattle; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D009637:Masoprocol / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology; D011565:Psoriasis / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D016859:Lipoxygenase Inhibitors; D009637:Masoprocol; D000875:Anthralin