(Carboxyalkyl) benzyl propargyl ethers as selective inhibitors of leukocyte-type 12-lipoxygenases

…, L Kuhnert, CR Johnson, LJ Marnett

文献索引：Gorins, Gilles; Kuhnert, Lethea; Johnson, Carl R.; Marnett, Lawrence J. Journal of Medicinal Chemistry, 1996 , vol. 39, # 25 p. 4871 - 4878

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被引用次数: 25

摘要

A series of (carboxyalkyl) benzyl propargyl ethers was synthesized and tested as inhibitors of 12-lipoxygenase (12-LO) from porcine leukocyte cytosol. Optimum activity was displayed by 3-[4-[(2-tridecynyloxy) methyl] phenyl] propanoic acid. Altering the length of the alkyl side chain attached to the acetylenic group reduced activity. Changing the substitution pattern in the (carboxyalkyl) benzyl group from para to meta or ortho also reduced activity. Analogs ...