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

M Lehr; M Klimt; A S Elfringhoff

doi:10.1016/s0960-894x(01)00472-3

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

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2569-72. doi: 10.1016/s0960-894x(01)00472-3.

Authors

M Lehr¹, M Klimt, A S Elfringhoff

Affiliation

¹ Institute of Pharmaceutical Chemistry, University of Münster, Hittorfstrasse 58-62, D-48149 Münster, Germany. lehrm@uni-muenster.de

PMID: 11551751
DOI: 10.1016/s0960-894x(01)00472-3

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 A(2). One of the most active compounds obtained was 26 with an IC(50) of 0.44 microM.

MeSH terms

Arachidonic Acid / metabolism
Blood Platelets / drug effects
Blood Platelets / metabolism
Cytosol / enzymology
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Humans
Indoles / chemical synthesis*
Indoles / pharmacology
Inhibitory Concentration 50
Phospholipases A / antagonists & inhibitors*

Substances

3-dodecanoylindole-2-carboxylic acid
Enzyme Inhibitors
Indoles
Arachidonic Acid
Phospholipases A