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Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity

Title
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity
Authors
Kang D.-H.Jun K.-Y.Jin P.L.Chwang S.P.Na Y.Kwon Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2009
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 52, no. 9, pp. 3093 - 3097
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of 3-acetyl-2-aminoquinolin-4-one derivatives selected from the Korean Chemical Bank were screened for calpain inhibitory activity by using a high-throughput fluorimetric calpain assay. We identified a potent and selective μ-calpain inhibitor, compound 17, whose specificity and efficacy for μ-calpain inhibition was better than MDL28170. Docking studies revealed that the efficacy of its inhibitory effect on calpain depended on the size and charge properties of the substitutions on the phenylamino ring. © 2009 American Chemical Society.
DOI
10.1021/jm8014734
Appears in Collections:
약학대학 > 약학과 > Journal papers
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