Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors

…, SH Seo, YH Lee, HD Kim, MH Son, BY Chung…

Index: Kwang, Seob Lee; Seon, Hee Seo; Yong, Ha Lee; Ha, Dong Kim; Moon, Ho Son; Bong, Young Chung; Jae, Yeol Lee; Jin, Changbae; Yong, Sup Lee Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 11 p. 2857 - 2860

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Citation Number: 44

Abstract

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 ...