title: Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A(2) enzymes.
abstract: A variety of 2-oxoamides and related amides based on natural and non-natural amino acids were synthesized. Their activity on two human intracellular phospholipases (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase (GV sPLA(2)) was evaluated. We show that an amide based on (R)-gamma-norleucine is a highly selective inhibitor of GV sPLA(2).
authors.affiliation: Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece.
authors.forename: Georgia
authors.initials: G
authors.lastname: Antonopoulou
authors.forename: Efrosini
authors.initials: E
authors.lastname: Barbayianni
authors.forename: Victoria
authors.initials: V
authors.lastname: Magrioti
authors.forename: Naomi
authors.initials: N
authors.lastname: Cotton
authors.forename: Daren
authors.initials: D
authors.lastname: Stephens
authors.forename: Violetta
authors.initials: V
authors.lastname: Constantinou-Kokotou
authors.forename: Edward A
authors.initials: EA
authors.lastname: Dennis
authors.forename: George
authors.initials: G
authors.lastname: Kokotos
mesh_terms: D000577:Amides / Q000737:chemistry; D000596:Amino Acids / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D064801:Phospholipase A2 Inhibitors; D054467:Phospholipases A2 / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000596:Amino Acids; D004791:Enzyme Inhibitors; D064801:Phospholipase A2 Inhibitors; D011725:Pyridines; C034960:oxoamide; D054467:Phospholipases A2