3-(3,5-Dimethyl-4-octadecanoylpyrrol-2-yl)propionic acids as inhibitors of 85 kDa cytosolic phospholipase A2

Article abstract of DOI:10.1002/ardp.19963291103

3-(1,4-Diacylpyrrol-2-yl)propionic acids were designed as inhibitors of cytosolic phospholipase A₂. 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]propio nic 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 A₂ (IC₅₀: 24 μM and 13 μM, respectively).