1422166-45-7Relevant academic research and scientific papers
Design, synthesis and cellular characterization of a dual inhibitor of 5-lipoxygenase and soluble epoxide hydrolase
Meirer, Karin,Glatzel, Daniel,Kretschmer, Simon,Wittmann, Sandra K.,Hartmann, Markus,Bl?cher, René,Angioni, Carlo,Geisslinger, Gerd,Steinhilber, Dieter,Hofmann, Bettina,Fürst, Robert,Proschak, Ewgenij
, (2017)
The arachidonic acid cascade is a key player in inflammation, and numerous well-established drugs interfere with this pathway. Previous studies have suggested that simultaneous inhibition of 5-lipoxygenase (5-LO) and soluble epoxide hydrolase (sEH) results in synergistic anti-inflammatory effects. In this study, a novel prototype of a dual 5-LO/sEH inhibitor KM55 was rationally designed and synthesized. KM55 was evaluated in enzyme activity assays with recombinant enzymes. Furthermore, activity of KM55 in human whole blood and endothelial cells was investigated. KM55 potently inhibited both enzymes in vitro and attenuated the formation of leukotrienes in human whole blood. KM55 was also tested in a cell function-based assay. The compound significantly inhibited the LPS-induced adhesion of leukocytes to endothelial cells by blocking leukocyte activation.
Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase
Meirer, Karin,R?dl, Carmen B.,Wisniewska, Joanna M.,George, Sven,H?fner, Ann-Kathrin,Buscató, Estella,Klingler, Franca-Maria,Hahn, Steffen,Berressem, Dirk,Wittmann, Sandra K.,Steinhilber, Dieter,Hofmann, Bettina,Proschak, Ewgenij
supporting information, p. 1777 - 1781 (2013/03/29)
Current research leads to the assumption that drugs affecting more than one target could result in a more efficient treatment of diseases and fewer safety concerns. Administration of drugs inhibiting only one branch of the arachidonic acid cascade is usua
