The pyrrole moiety as a template for COX-1/COX-2 inhibitors

G Dannhardt, W Kiefer, G Krämer, S Maehrlein…

文献索引：Dannhardt, Gerd; Kiefer, Werner; Kraemer, Godehard; Maehrlein, Sabine; Nowe, Ulrike; Fiebich, Bernd European Journal of Medicinal Chemistry, 2000 , vol. 35, # 5 p. 499 - 510

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被引用次数: 164

摘要

Aroyl-and thiophene-substituted pyrrole derivatives have been synthesized as a new class of COX-1/COX-2 inhibitors. The inhibition of COX-1 was evaluated in a biological system using bovine PMNLs as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of the concentration of arachidonic acid metabolites was performed by HPLC for COX-1 and RIA for COX-2. ...