Source:http://linkedlifedata.com/resource/pubmed/id/21504847
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
|
pubmed:dateCreated |
2011-5-2
|
pubmed:abstractText |
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 ?-position, showed potent ?-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 ?-calpain (IC(50)=0.13 ?M) and also exhibited strong antioxidant activities in DPPH and superoxide anion radical scavenging and lipid peroxidation inhibition assay systems.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Antioxidants,
http://linkedlifedata.com/resource/pubmed/chemical/Cinnamates,
http://linkedlifedata.com/resource/pubmed/chemical/Glycoproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Ketones,
http://linkedlifedata.com/resource/pubmed/chemical/calpain inhibitors
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
1464-3405
|
pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
21
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2850-4
|
pubmed:meshHeading |
pubmed-meshheading:21504847-Amides,
pubmed-meshheading:21504847-Antioxidants,
pubmed-meshheading:21504847-Binding Sites,
pubmed-meshheading:21504847-Cinnamates,
pubmed-meshheading:21504847-Crystallography, X-Ray,
pubmed-meshheading:21504847-Enzyme Activation,
pubmed-meshheading:21504847-Glycoproteins,
pubmed-meshheading:21504847-Inhibitory Concentration 50,
pubmed-meshheading:21504847-Ketones,
pubmed-meshheading:21504847-Models, Molecular,
pubmed-meshheading:21504847-Molecular Structure
|
pubmed:year |
2011
|
pubmed:articleTitle |
Synthesis of cinnamoyl ketoamides as hybrid structures of antioxidants and calpain inhibitors.
|
pubmed:affiliation |
Department of Pharmaceutical Science, College of Pharmacy Kyung Hee University, Seoul 130-701, Republic of Korea.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|