新型人IVA组磷脂酶A(2)的2-氧代酰胺抑制剂
Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2).
作者信息
Kokotos George, Kotsovolou Stavroula, Six David A, Constantinou-Kokotou Violetta, Beltzner Christopher C, Dennis Edward A
机构信息
Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece.
出版信息
J Med Chem. 2002 Jul 4;45(14):2891-3. 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 PLA(2) activity at 0.009 mole fraction.
开发了一类新型的强效人胞质磷脂酶A(2)(GIVA PLA(2))抑制剂。这些抑制剂被设计成含有2-氧代酰胺官能团和一个游离羧基。在测试的化合物中，含有L-γ-正亮氨酸的长链2-氧代酰胺是最有效的抑制剂，在0.009摩尔分数时使GIVA PLA(2)活性降低50%。
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