Nonsteroidal antiinflammatory agents, XVII: Inhibition of bovine cyclooxygenase and 5-lipoxygenase by N-alkyldiphenyl-pyrrolyl acetic and propionic acid derivatives.
A series of 19 N-alkyl-diarylpyrrolyl-acetic and-propionic acid derivatives was synthesized and tested. Using bovine blood as enzyme source the inhibition of cyclooxygenase and 5-lipoxygenase, respectively, was applied to determine the antiinflammatory activity. In general all compounds tested inhibit 5-lipoxygenase more effectively than cyclooxygenase. A structure-activity relationship is discussed.
Dannhardt
G
G
Institut für Pharmazeutische Chemie der Johann Wolfgang Goethe-Universität, Frankfurt, Germany.
Lehr
M
M
D000085:Acetates / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001792:Blood Platelets / Q000201:enzymology; D002417:Cattle; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D009504:Neutrophils / Q000201:enzymology; D011422:Propionates / Q000138:chemical synthesis* / Q000494:pharmacology
D000085:Acetates; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; D011422:Propionates