125197-89-9Relevant academic research and scientific papers
Design, Synthesis, and 5-Lipoxygenase-Inhibiting Properties of 1-Thio-Substiuted Butadienes
Hanko, Rudolf,Hammond, Michael D.,Fruchtmann, Romanis,Pfitzner, Joerg,Place, Graham A.
, p. 1163 - 1170 (2007/10/02)
The synthesis of novel 1-thio-substituted butadienes, designed as mechanism-based 5-lipoxygenase inhibitors, is described.The structure of these compounds closely resembles a proposed high-energy intermediate during the lipoxygenation of arachidonic acid.They demonstrate 5-lipoxygenase inhibition in vitro and in vivo.The most potent compound is 15a with an IC50 of μM in vitro.LTC4 release was inhibited by 80percent after intraperitoneal administration of 15c at a dose of 2 mg/kg.
