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

, : The pyrrole moiety as a template for COX-1/COX-2 inhibitors. European Journal of Medicinal Chemistry 35(5): 499-510, May

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. Variation of the substitution pattern led to a series of active compounds which showed inhibition for COX-1 and COX-2. Structural requirements for the development of COX-1/COX-2 inhibitors are discussed.


PMID: 10889329

DOI: 10.1016/s0223-5234(00)00150-1

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