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

نویسندگان

  • George Kokotos
  • Stavroula Kotsovolou
  • David A Six
  • Violetta Constantinou-Kokotou
  • Christopher C Beltzner
  • Edward A Dennis
چکیده

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 PLA(2) activity at 0.009 mole fraction.

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عنوان ژورنال:
  • Journal of medicinal chemistry

دوره 45 14  شماره 

صفحات  -

تاریخ انتشار 2002