Synthesis of 2-oxoamides based on delta-amino acids and study of their activity on human GIVA phospholipase A_2

摘要

The Group IVA cytosolic phospholipase A_2(GIVA PLA_2)is a particularly attractive target for drug development since it is the rate-limiting provider of proinflammatory mediators.We have previously reported the discovery of novel 2-oxoamides based on gamma-amino acids that inhibit GIVA PLA_2.Here,we present our results on the synthesis of 2-oxoamides based on 5-amino acids and the study of their activity on human GIVA PLA_2.