Cyclooxygenase-1/2 (COX-1/COX-2) and 5-lipoxygenase (5-LOX) inhibitors of the 6, 7-diaryl-2, 3-1H-dihydropyrrolizine type

H Ulbrich, B Fiebich, G Dannhardt

文献索引：Ulbrich, Holger; Fiebich, Bernd; Dannhardt, Gerd European Journal of Medicinal Chemistry, 2002 , vol. 37, # 12 p. 953 - 959

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被引用次数: 57

摘要

A series of 6, 7-diaryl-2, 3-1H-dihydropyrrolizines was prepared as COX-1/COX-2 and 5- LOX inhibitors. The inhibition of COX-1 was evaluated using intact bovine platelets as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of arachidonic metabolites was performed by HPLC for COX-1 and RIA for COX-2. The balance between COX-1/COX-2 and 5-LOX inhibition ...