1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α: Bioisosteric replacement of the carboxylic acid and carboxamide moiety
Indole-5-carboxylic acids and -carboxamides with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent inhibitors of cytosolic phospholipase A2α (cPLA2α) isolated from human platelets. In continuation of
Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2α
The synthesis and structure-activity relationship study of a series of 1-indol-1-yl-3-phenoxypropan-2-one inhibitors of cytosolic phospholipase A 2α. (cPLA2α) are described. The compounds were evaluated in a vesicle assay with isolated cPLA2α and in cellular assays with intact human platelets. Systematic variation led to 3-methylhydrogen 1-[3-(4-decyloxyphenoxy)-2-oxopropyl]indole-3,5-dicarboxylate (57), which revealed the highest activity against the isolated enzyme. With an IC50 value of 4.3 nM in this assay, it is one of the most potent in vitro cPLA2α inhibitors known today.
NOVEL HETEROARYL-SUBSTITUTED ACETONE DERIVATIVES AS INHIBITORS OF PHOSPHOLIPASE A2
The invention relates to novel heteroaryl-substituted acetone derivatives, which inhibit the enzyme phospholipase A2, to pharmaceutical agents that contain said compounds and to a method for producing said compounds.
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(2008/06/13)
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