3‐(3,5‐Dimethyl‐4‐octadecanoylpyrrol‐2‐yl)propionic Acids as Inhibitors of 85 kDa Cytosolic Phospholipase A 2 | Zendy

Lehr Matthias | Zendy

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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).

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