Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors
- Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors
- 유영재; 남동혁; 정서윤; 장재완; 김형자; 진창배; 배애님; 이용섭
- Calpain inhibitor; Cell death; Cinnamoyl ketoamides; Docking; Antioxidant
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 21, NO 10, 2850-2854
- The excessive calpain activation causes serious cellular damage or even cell death in neurological disorders
such as stroke and Alzheimer’s disease. Oxidative stress has also been implicated in the initiation or
progression of neurodegenerative diseases. In the present studies, a series of cinnamoyl ketoamides 4a–
4j were synthesized as hybrid structures of antioxidants and calpain inhibitors. Cinnamoyl ketoamides,
possessing an alkyl chain at the α-position, showed potent μ-calpain inhibitory activities indicating that
the cinnamoyl skeleton can be regarded as an acyclic variant of calpain inhibitory chromone carboxamide
2. Among synthesized, compound 4e was the most potent inhibitor of l-calpain (IC50 = 0.13 μM) and also
exhibited strong antioxidant activities in DPPH and superoxide anion radical scavenging and lipid peroxidation
inhibition assay systems.
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