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dc.contributor.authorKim, Sang Hoon-
dc.contributor.authorLee, Young Hoon-
dc.contributor.authorJung, Seo Yun-
dc.contributor.authorKim, Hyoung Ja-
dc.contributor.authorJin, Changbae-
dc.contributor.authorLee, Yong Sup-
dc.date.accessioned2024-01-20T17:04:01Z-
dc.date.available2024-01-20T17:04:01Z-
dc.date.created2021-09-02-
dc.date.issued2011-05-
dc.identifier.issn0223-5234-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/130421-
dc.description.abstractThe 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.-
dc.languageEnglish-
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER-
dc.subjectMOUSE MODEL-
dc.subjectDISEASE-
dc.subjectACTIVATION-
dc.subjectAPOPTOSIS-
dc.subjectSTRESS-
dc.subjectDESIGN-
dc.subjectSYSTEM-
dc.subjectRATS-
dc.titleSynthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties-
dc.typeArticle-
dc.identifier.doi10.1016/j.ejmech.2011.02.025-
dc.description.journalClass1-
dc.identifier.bibliographicCitationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.5, pp.1721 - 1728-
dc.citation.titleEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY-
dc.citation.volume46-
dc.citation.number5-
dc.citation.startPage1721-
dc.citation.endPage1728-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000289655100030-
dc.identifier.scopusid2-s2.0-79953171480-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.type.docTypeArticle-
dc.subject.keywordPlusMOUSE MODEL-
dc.subject.keywordPlusDISEASE-
dc.subject.keywordPlusACTIVATION-
dc.subject.keywordPlusAPOPTOSIS-
dc.subject.keywordPlusSTRESS-
dc.subject.keywordPlusDESIGN-
dc.subject.keywordPlusSYSTEM-
dc.subject.keywordPlusRATS-
dc.subject.keywordAuthorCalpain inhibitor-
dc.subject.keywordAuthorCell death-
dc.subject.keywordAuthorNeurodegenerative disease-
dc.subject.keywordAuthorChromone carboxamide-
dc.subject.keywordAuthorAntioxidant-
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