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RESEARCH PRODUCT
Synthesis and Evaluation of a Novel Series of Pyrrolizine Derivatives as Dual Cyclooxygenase-1 and 5-Lipoxygenase Inhibitors
Susanne TriesGerd DannhardtT. KammermeierStefan LauferHans-günter StriegelWerner KieferKarola NeherCornelia DonatSibylle BaurPia ZechmeisterKatrin Stolingwasubject
Blood PlateletsMaleNeutrophilsmedicine.drug_classPharmaceutical ScienceContext (language use)Monoclonal antibodyChemical synthesisDrug DiscoverymedicineHumansStructure–activity relationshipCyclooxygenase InhibitorsPyrrolesLipoxygenase InhibitorsWhole bloodArachidonate 5-LipoxygenasebiologyChemistryMembrane ProteinsIn vitroIsoenzymesBiochemistryProstaglandin-Endoperoxide SynthasesEnzyme inhibitorArachidonate 5-lipoxygenaseCyclooxygenase 1biology.proteinFemaledescription
The aim of our study was to investigate structure activity relationship following the replacement of the 6-phenyl substituent at the 6,7-diaryl-2,3-dihydropyrrolizine template by various heteroaromatic residues. In this context we developed a new, efficient, and highly sensitive test method for the screening of dual cyclooxygenase-1 (COX-1) and 5-lipoxygenase (5-LOX) inhibitors. We used human platelets as a source of COX-1 and human PMNLs as a source of 5-LOX. Both cell types were isolated from the same volume of blood. PGE2 and LTB4 respectively were determined by highly selective and sensitive ELISA kits, using monoclonal antibodies. For a single determination at most 0.5 mL whole blood is needed.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1997-12-13 | Archiv der Pharmazie |