Excessive calpain activations contribute to serious cellular damage and have been found in many pathological conditions. Novel chromone carboxamides derived from ketoamides were prepared and evaluated for μ-calpain inhibition. Among synthesized, compound 2i was the most potent calpain inhibitor with an IC50 value of 0.24±0.11 μM comparable to the activity of peptide aldehyde calpain inhibitor MDL 28,170. Furthermore, compound 2i ...