Bioorganic & Medicinal Chemistry Letters 2001-10-08

Novel 3-dodecanoylindole-2-carboxylic acid inhibitors of cytosolic phospholipase A(2).

M Lehr, M Klimt, A S Elfringhoff

文献索引：Bioorg. Med. Chem. Lett. 11(19) , 2569-72, (2001)

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摘要

Derivatives of 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) with modified substituents at the indole-1-position were synthesized and evaluated for their ability to inhibit the arachidonic acid release in human platelets mediated by the cytosolic phospholipase A(2). One of the most active compounds obtained was 26 with an IC(50) of 0.44 microM.