Synthesis of 2-oxoamides based on sulfonamide analogs of γ-amino acids and their activity on phospholipase A2

A variety of lipophilic 2‐oxoamides containing sulfonamide analogs of γ‐amino acids as well as acyl sulfonamides of γ‐aminobutyric acid were synthesized. Their ability to inhibit intracellular GIVA cPLA2 and GVIA iPLA2 as well as secreted GV sPLA2 was evaluated. The sulfonamide group seems a bioisos...

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Published inJournal of peptide science Vol. 14; no. 10; pp. 1111 - 1120
Main Authors Antonopoulou, Georgia, Magrioti, Victoria, Stephens, Daren, Constantinou-Kokotou, Violetta, Dennis, Edward A., Kokotos, George
Format Journal Article
LanguageEnglish
Published Chichester, UK John Wiley & Sons, Ltd 01.10.2008
Subjects
2-oxoamides
acyl sulfonamides
Amino Acids - chemistry
Amino Acids - physiology
Humans
inhibitors
Isoenzymes - antagonists & inhibitors
Isoenzymes - metabolism
phospholipase A2
Phospholipase A2 Inhibitors
Phospholipases A2 - metabolism
Pyridines - chemical synthesis
Pyridines - pharmacology
sulfonamides
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Summary:A variety of lipophilic 2‐oxoamides containing sulfonamide analogs of γ‐amino acids as well as acyl sulfonamides of γ‐aminobutyric acid were synthesized. Their ability to inhibit intracellular GIVA cPLA2 and GVIA iPLA2 as well as secreted GV sPLA2 was evaluated. The sulfonamide group seems a bioisosteric group suitable to replace the carboxyl group in 2‐oxoamide inhibitors of GVIA cPLA2. Copyright © 2008 European Peptide Society and John Wiley & Sons, Ltd.
Bibliography:NIH - No. GM 20,501
istex:2D6C455EA5776933D90F457B13E3F4C6B68D17C0
ArticleID:PSC1048
AnalgesiX/UC Discovery Biotechnology - No. B1002-10303
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ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ObjectType-Article-1
ObjectType-Feature-2
ISSN:1075-2617
1099-1387
DOI:10.1002/psc.1048