Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A(2) 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)-gam...

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Published inBioorganic & medicinal chemistry Vol. 16; no. 24; pp. 10257 - 10269
Main Authors Antonopoulou, Georgia, Barbayianni, Efrosini, Magrioti, Victoria, Cotton, Naomi, Stephens, Daren, Constantinou-Kokotou, Violetta, Dennis, Edward A, Kokotos, George
Format Journal Article
LanguageEnglish
Published England 15.12.2008
Subjects
Amides - chemistry
Amino Acids - chemistry
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Molecular Structure
Phospholipase A2 Inhibitors
Phospholipases A2 - pharmacology
Pyridines - chemistry
Structure-Activity Relationship
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Summary: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).
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:1464-3391
DOI:10.1016/j.bmc.2008.10.046