Smyrniotou A1, Kokotou MG2, Mouchlis VD3, Barbayianni E4, Kokotos G4, Dennis EA5, Constantinou-Kokotou V6.
Bioorg Med Chem. 2016 Dec 8. pii: S0968-0896(16)31374-8. doi: 10.1016/j.bmc.2016.12.007. [Epub ahead of print]Calcium-independent phospholipase A2 (GVIA iPLA2) has recently attracted interest as a medicinal target. The number of known GVIA iPLA2 inhibitors is limited to a handful of synthetic compounds (bromoenol lactone and polyfluoroketones). To expand the chemical diversity, a variety of 2-oxoamides based on dipeptides and ether dipeptides were synthesized and studied for their in vitro inhibitory activity on human GVIA iPLA2 and their selectivity over the other major intracellular GIVA cPLA2 and the secreted GV sPLA2. Read More