174347-75-2Relevant academic research and scientific papers
Synthesis and evaluation of a novel series of pyrrolizine derivatives as dual cyclooxygenase-1 and 5-lipoxygenase inhibitors
Laufer, Stefan,Striegel, Hans-Guenter,Neher, Karola,Zechmeister, Pia,Donat, Cornelia,Stolingwa, Katrin,Baur, Sibylle,Tries, Susanne,Kammermeier, Thomas,Dannhardt, Gerd,Kiefer, Werner
, p. 307 - 312 (2007/10/03)
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.
