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

…, L Kuhnert, CR Johnson, LJ Marnett

Index: 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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Citation Number: 25

Abstract

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 ...