title: Synthesis of lipidic amino acid and dipeptide inhibitors of human platelet phospholipase A2.
abstract: Phospholipases A2 (PLA2s) catalyze the hydrolysis of glycerophospholipids at the sn-2 position, and their inhibition is considered a rational approach for the prevention and treatment of inflammation. A number of amides and esters of alpha-amino acids with saturated linear side chains, esters of alpha-amino alcohols and derivatives of lipidic peptides were prepared and tested against secreted humal platelet phospholipase A2. Among the compounds tested the amides of free amino acids with long-chain amines presented the highest in vitro inhibitory activity.
authors.affiliation: Department of Chemistry, University of Athens, Greece.
authors.forename: G
authors.initials: G
authors.lastname: Kokotos
authors.forename: V
authors.initials: V
authors.lastname: Constantinou-Kokotou
authors.forename: C
authors.initials: C
authors.lastname: Noula
authors.forename: A
authors.initials: A
authors.lastname: Nicolaou
authors.forename: W A
authors.initials: WA
authors.lastname: Gibbons
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D001792:Blood Platelets / Q000201:enzymology*; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010712:Phosphatidic Acids / Q000378:metabolism*; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D054467:Phospholipases A2; D016339:Spectrometry, Mass, Fast Atom Bombardment
chemical_list: D000596:Amino Acids; D004151:Dipeptides; D004791:Enzyme Inhibitors; D010712:Phosphatidic Acids; D010741:Phospholipases A; D054467:Phospholipases A2