Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2)

作者：Kokotos G^*; Kotsovolou S; Six DA; Constantinou Kokotou V; Beltzner CC; Dennis EA

来源：Journal of Medicinal Chemistry, 2002, 45(14): 2891-2893.

DOI：10.1021/jm025538p

A novel class of potent human cytosolic phospholipase A(2) (GIVA PLA(2)) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a long-chain 2-oxoamide containing L-gamma-norleucine was the most potent inhibitor, causing a 50% decrease in GIVA PLA2 activity at 0.009 mole fraction.

• 出版日期2002-7-4