Synthesis and Evaluation of a Novel Series of Pyrrolizine Derivatives as Dual Cyclooxygenase-1 and 5-Lipoxygenase Inhibitors
| Autor: | Susanne Tries, Gerd Dannhardt, T. Kammermeier, Stefan Laufer, Hans-Günter Striegel, Werner Kiefer, Karola Neher, Cornelia Donat, Sibylle Baur, Pia Zechmeister, Katrin Stolingwa |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
Blood Platelets
Male Neutrophils medicine.drug_class Pharmaceutical Science Context (language use) Monoclonal antibody Chemical synthesis Drug Discovery medicine Humans Structure–activity relationship Cyclooxygenase Inhibitors Pyrroles Lipoxygenase Inhibitors Whole blood Arachidonate 5-Lipoxygenase biology Chemistry Membrane Proteins In vitro Isoenzymes Biochemistry Prostaglandin-Endoperoxide Synthases Enzyme inhibitor Arachidonate 5-lipoxygenase Cyclooxygenase 1 biology.protein Female |
| Zdroj: | Archiv der Pharmazie. 330:307-312 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.19973300908 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text