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

Citation:

Antonopoulou G, Magrioti V, Stephens D, Constantinou-Kokotou V, Dennis EA, Kokotos G. Synthesis of 2-oxoamides based on sulfonamide analogs of gamma-amino acids and their activity on phospholipase A2. Journal of Peptide Science. 2008;14(10):1111-1120.

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 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.