6533b82afe1ef96bd128c219
RESEARCH PRODUCT
The pyrrole moiety as a template for COX-1/COX-2 inhibitors
Gerd DannhardtSabine MaehrleinGodehard KrämerGodehard KrämerUlrike NoweWerner KieferBernd L. Fiebichsubject
DiclofenacNeutrophilsStereochemistryIndomethacinThiophenesHigh-performance liquid chromatographyMonocytesPyrrole derivativeschemistry.chemical_compoundDrug DiscoveryAnimalsHumansStructure–activity relationshipMoietyCyclooxygenase InhibitorsPyrrolesSulfonesPyrrolePharmacologychemistry.chemical_classificationArachidonic AcidCyclooxygenase 2 InhibitorsMolecular StructureAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryMembrane ProteinsGeneral MedicineIsoenzymesEnzymechemistryMembrane proteinBiochemistryCyclooxygenase 2Prostaglandin-Endoperoxide SynthasesCyclooxygenase 1Leukocytes MononuclearCattleArachidonic aciddescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2000-07-12 | European Journal of Medicinal Chemistry |