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Synthesis of lipophilic 2-oxoamides based on γ-aminobutyric and δ-aminovaleric analogues and their activity against phospholipase A2

✍ Scribed by Panagiota Moutevelis-Minakakis; Afroditi Neokosmidi; Maria Filippakou; Daren Stephens; Edward A. Dennis; George Kokotos

Publisher: John Wiley and Sons
Year: 2007
Tongue: English
Weight: 170 KB
Volume: 13
Category: Article
ISSN: 1075-2617
DOI: 10.1002/psc.889

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✦ Synopsis

Abstract

A variety of lipophilic 2‐oxoamides based on γ‐aminobutyric and δ‐aminovaleric analogues were synthesized. 2‐oxoamides containing a tetrazole, a thioethyl or a thioacetyl group are weak inhibitors of GIVA cPLA~2~, while derivatives containing a methyl tetrazole, a diethyl phosphonate or a thioethyl group are weak inhibitors of GV sPLA~2~. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd.

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Synthesis of 2-oxoamides based on sulfon

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

✍ Georgia Antonopoulou; Victoria Magrioti; Daren Stephens; Violetta Constantinou-K 📂 Article 📅 2008 🏛 John Wiley and Sons 🌐 English ⚖ 170 KB

## 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 gr