Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors

Title
Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors
Authors
유영재남동혁정서윤장재완김형자진창배배애님이용섭
Keywords
Calpain inhibitor; Cell death; Cinnamoyl ketoamides; Docking; Antioxidant
Issue Date
2011-05
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 21, NO 10, 2850-2854
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/39788
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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