Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes

Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes

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 )-γ-...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-12, Vol.16 (24), p.10257-10269
Hauptverfasser: ANTONOPOULOU, Georgia, BARBAYIANNI, Efrosini, MAGRIOTI, Victoria, COTTON, Naomi, STEPHENS, Daren, CONSTANTINOU-KOKOTOU, Violetta, DENNIS, Edward A, KOKOTOS, George
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Medical sciences
Pharmacology. Drug treatments
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Zusammenfassung: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 )-γ-norleucine is a highly selective inhibitor of GV sPLA 2 .
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.10.046