Synthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties

Authors
Kim, Sang HoonLee, Young HoonJung, Seo YunKim, Hyoung JaJin, ChangbaeLee, Yong Sup
Issue Date
2011-05
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.5, pp.1721 - 1728
Abstract
The overactivation of mu-calpain can cause serious cell damage in several diseases. Furthermore, cell death in a number of neurodegenerative disorders is linked to the overproduction of reactive oxygen species. Therefore, antioxidants and mu-calpain inhibitors could have the therapeutic potentials to treat cell death related diseases. New chromone carboxamide derivatives 3 were synthesized to provide alternative mu-calpain inhibitors to compound 2, a conformationally constrained structural variant of MDL 28,170. Compounds 3h and 3l exhibited the most potent p-calpain inhibitory activities (IC50 = 0.09-0.10 mu M), and were comparable to 2 in this respect (IC50 = 0.07 mu M). Compound 31 showed both potent p-calpain inhibitory activity (IC50 = 0.28 mu M) and antioxidant activities in DPPH scavenging and lipid peroxidation inhibition assays. (C) 2011 Elsevier Masson SAS. All rights reserved.
Keywords
MOUSE MODEL; DISEASE; ACTIVATION; APOPTOSIS; STRESS; DESIGN; SYSTEM; RATS; MOUSE MODEL; DISEASE; ACTIVATION; APOPTOSIS; STRESS; DESIGN; SYSTEM; RATS; Calpain inhibitor; Cell death; Neurodegenerative disease; Chromone carboxamide; Antioxidant
ISSN
0223-5234
URI
https://pubs.kist.re.kr/handle/201004/130421
DOI
10.1016/j.ejmech.2011.02.025
Appears in Collections:
KIST Article > 2011
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