Cyclooxygenase-1/2 (COX-1/COX-2) and 5-lipoxygenase (5-LOX) inhibitors of the 6,7-diaryl-2,3-1H-dihydropyrrolizine type
| Autor: | Holger Ulbrich, Gerd Dannhardt, Bernd L. Fiebich |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Blood Platelets
Radioimmunoassay High-performance liquid chromatography Isozyme Monocytes Drug Discovery medicine Cox 1 cox 2 Animals Humans Moiety Structure–activity relationship Pyrroles Platelet Lipoxygenase Inhibitors Enzyme Inhibitors Chromatography High Pressure Liquid Pharmacology chemistry.chemical_classification biology Chemistry Organic Chemistry Membrane Proteins General Medicine In vitro Isoenzymes medicine.anatomical_structure Enzyme Biochemistry Cyclooxygenase 2 Prostaglandin-Endoperoxide Synthases Enzyme inhibitor Drug Design Arachidonate 5-lipoxygenase Cyclooxygenase 1 biology.protein Cattle Cyclooxygenase Nucleus |
| Zdroj: | European Journal of Medicinal Chemistry. 37:953-959 |
| ISSN: | 0223-5234 |
| Popis: | 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 can be shifted by modifying the substitution pattern of the phenyl moiety at the 6- and 7-position of the pyrrolizine nucleus. Structure-activity relationships are discussed. |
| Databáze: | OpenAIRE |
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