SYNTHESIS OF LIPIDIC AMINO-ACID AND DIPEPTIDE INHIBITORS OF HUMAN PLATELET PHOSPHOLIPASE A(2)

Phospholipases A(2) (PLA(2)s) catalyze the hydrolysis of glycerophosph olipids at the sn-2 position, and their inhibition is considered a rat ional approach for the prevention and treatment of inflammation. A num ber of amides and esters of alpha-amino acids with saturated linear si de chains, esters of alpha-amino alcohols and derivatives of lipidic p eptides were prepared and tested against secreted humal platelet phosp holipase A(2). Among the compounds tested the amides of free amino aci ds with long-chain amines presented the highest in vitro inhibitory ac tivity. (C) Munksgaard 1996.