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

Bioorganic & medicinal chemistry letters (2001-09-12)
M Lehr, M Klimt, A S Elfringhoff
RÉSUMÉ

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.