Kim, Sang Hoon Lee, Young Hoon Jung, Seo Yun Kim, Hyoung Ja Jin, Changbae Lee, Yong Sup 2024-01-20T17:04:01Z 2024-01-20T17:04:01Z 2021-09-02 2011-05 0223-5234 https://pubs.kist.re.kr/handle/201004/130421 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. English ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER MOUSE MODEL DISEASE ACTIVATION APOPTOSIS STRESS DESIGN SYSTEM RATS Synthesis of chromone carboxamide derivatives with antioxidative and calpain inhibitory properties Article 10.1016/j.ejmech.2011.02.025 1 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.5, pp.1721 - 1728 EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 46 5 1721 1728 scie scopus 000289655100030 2-s2.0-79953171480 Chemistry, Medicinal Pharmacology & Pharmacy Article MOUSE MODEL DISEASE ACTIVATION APOPTOSIS STRESS DESIGN SYSTEM RATS Calpain inhibitor Cell death Neurodegenerative disease Chromone carboxamide Antioxidant