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3‐(Octadecanoylaminomethyl)indole‐2‐carboxylic Acid Derivatives and 1‐Methyl‐3‐octadecanoylindole‐2‐carboxylic Acid as Inhibitors of Cytosolic Phospholipase A 2
Author(s) -
Lehr Matthias
Publication year - 1996
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19963290803
Subject(s) - carboxylic acid , chemistry , indole test , phospholipase a2 , arachidonic acid , cytosol , enzyme , ionophore , biochemistry , stereochemistry , membrane
3‐(1‐Acylaminooctadecyl)indole‐2‐carboxylic acids and 3‐(1‐acylaminooctadecyl)‐1‐methylindole‐2‐carboxylic acids were designed and synthesized as inhibitors of cytosolic phospholipase A 2 . Enzyme inhibition was assayed by evaluation of calcium ionophore A23187‐induced arachidonic acid release from bovine platelets. While compounds with 1‐octadecanoylaminooctadecyl groups in position 3 of the indole were inactive inhibition data for 3‐[1‐(3‐phenylpropionylamino)octadecyl]indole‐2‐carboxylic acids could not be evaluated because of lysis of the platelets. However 3‐(octadecanoylaminomethyl)indole‐2‐carboxylic acid derivatives and 1‐methyl‐3‐octadecanoylindole‐2‐carboxylic acid proved to be inhibitors of cytosolic phospholipase A 2 . The most active inhibitor was the latter compound with an IC 50 of 8 μM.