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

✍ Scribed by Georgia Antonopoulou; Victoria Magrioti; Daren Stephens; Violetta Constantinou-Kokotou; Edward A. Dennis; George Kokotos

Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
170 KB
Volume
14
Category
Article
ISSN
1075-2617

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✦ Synopsis

Abstract

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 cPLA~2~ and GVIA iPLA~2~ as well as secreted GV sPLA~2~ was evaluated. The sulfonamide group seems a bioisosteric group suitable to replace the carboxyl group in 2‐oxoamide inhibitors of GVIA cPLA~2~. Copyright © 2008 European Peptide Society and John Wiley & Sons, Ltd.

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