Premium
3‐(3,5‐Dimethyl‐4‐octadecanoylpyrrol‐2‐yl)propionic Acids as Inhibitors of 85 kDa 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.19963291103
Subject(s) - cytosol , arachidonic acid , chemistry , phospholipase a2 , phospholipase a , enzyme , ionophore , phospholipase , biochemistry , calcium , phospholipase c , enzyme inhibitor , stereochemistry , organic chemistry
3‐(1,4‐Diacylpyrrol‐2‐yl)propionic acids were designed 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 the synthesized bisacyl compound 3‐[3,5‐dimethyl‐4‐octadecanoyl‐1‐(3‐phenylpropionyl)pyrrol‐2‐yl]propionic acid was inactive at 33 μM, the related monoacylated 3‐(3,5‐dimethyl‐4‐octadecanoylpyrrol‐2‐yl)propionic acid and 3‐(1,3,5‐trimethyl‐4‐octadecanoylpyrrol‐2‐yl)propionic acid proved to be inhibitors of cytosolic phospholipase A 2 (IC 50 : 24 μM and 13 μM, respectively).