1007567-06-7Relevant academic research and scientific papers
Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitors
Nam, Dong Hyuk,Lee, Kwang Seob,Kim, Sang Hoon,Kim, Sung Min,Jung, Seo Yun,Chung, Sung Hyun,Kim, Hyoung Ja,Kim, Nam Doo,Jin, Changbae,Lee, Yong Sup
, p. 205 - 209 (2008/09/17)
Calpains are involved in a variety of calcium-regulated cellular processes, such as signal transduction, cell proliferation, differentiation, and apoptosis. Excessive calpain activation contributes to serious cellular damage and has been reported in many pathological conditions. 4-Quinolinone 2-carboxamide derivatives were prepared and evaluated for μ-calpain inhibitory activities. Of the compounds synthesized, 3a and 3k, which possess a primary amide and 4-methoxyphenethyl amide at P1′ region, were found to most potently inhibit μ-calpain with IC50 values of 0.71 ± 0.07 and 0.73 ± 0.23 μM, respectively. On the other hand, the incorporation of pyridine-containing amides decreased inhibitory activity.
