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European journal of medicinal chemistry

Synthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties.


PMID 21397369

Abstract

The overactivation of μ-calpain can cause serious cell damage in several diseases. Furthermore, cell death in a number of neurodegenerative disorders is linked to the overproduction of reactive oxygen species. Therefore, antioxidants and μ-calpain inhibitors could have the therapeutic potentials to treat cell death related diseases. New chromone carboxamide derivatives 3 were synthesized to provide alternative μ-calpain inhibitors to compound 2, a conformationally constrained structural variant of MDL 28,170. Compounds 3h and 3l exhibited the most potent μ-calpain inhibitory activities (IC50=0.09-0.10 μM), and were comparable to 2 in this respect (IC50=0.07 μM). Compound 3i showed both potent μ-calpain inhibitory activity (IC50=0.28 μM) and antioxidant activities in DPPH scavenging and lipid peroxidation inhibition assays.