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

基于γ-氨基酸磺酰胺类似物的2-氧代酰胺的合成及其对磷脂酶A2的活性

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Abstract

A variety of lipophilic 2-oxoamides containing sulfonamide analogs of gamma-amino acids as well as acyl sulfonamides of gamma-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.

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