期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 21, 页码 6384-6393出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.08.062
关键词
Ischemia/reperfusion; Mitochondrial swelling; Mitochondrial permeability transition (MPT); Cyclophilin A; Cyclophilin D; Dantrolene
资金
- Ministry of Education, Culture, Sports, Science and Technology [24790119]
- Grants-in-Aid for Scientific Research [24790119, 21790107, 22249006] Funding Source: KAKEN
A structure consisting of substituted hydantoin linked to a 5-(halophenyl)furan-2-yl group via an amide bond was identified as a promising scaffold for development of low-molecular-weight therapeutic agents to treat vascular dysfunction, including ischemia/reperfusion injury. Among the compounds synthesized, 5-(3,5-dichlorophenyl)-N-{2,4-dioxo-3-[(pyridin-3-yl)methyl]imidazolidin-1-yl}-2-furamide (17) possessed the most potent inhibitory activity against Ca2+-induced mitochondrial swelling. The structural development, synthesis and structure-activity relationship of these compounds are described. (C) 2012 Elsevier Ltd. All rights reserved.
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