期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 35, 期 5, 页码 499-510出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(00)00150-1
关键词
COX-1/COX-2 inhibition; pyrrole derivatives; enzyme selectivity; structure-activity relationship
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, (C) 2000 Editions scientifiques et medicales Elsevier SAS.
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