Bioorganic & medicinal chemistry letters

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

M Lehr, M Klimt, AS Elfringhoff

Index: Lehr, Matthias; Klimt, Monika; Elfringhoff, Alwine Schulze Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 19 p. 2569 - 2572

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Citation Number: 22

Abstract

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 A2. One of the most active compounds obtained was 26 with an IC50 of 0.44 μM.