Small-molecular inhibitors of Ca2+-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene |
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| Authors: | Shinpei Murasawa Katsuya Iuchi Shinichi Sato Tomomi Noguchi-Yachide Mikiko Sodeoka Tsutomu Yokomatsu Kosuke Dodo Yuichi Hashimoto Hiroshi Aoyama |
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| Affiliation: | 1. Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan;2. Sodeoka Live Cell Chemistry Project, ERATO, JST, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan;3. Advanced Science Institute (ASI), RIKEN, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan;4. Graduate School of Medicine, Nippon Medical School, 1-396 Kosugi-machi, Nakahara-ku, Kawasaki-city, Kanagawa 211-8533, Japan;5. Department of Chemistry, Faculty of Science, Gakushuin University, 1-5-1 Mejiro, Toshima-ku, Tokyo 171-8588, Japan;6. School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji-city, Tokyo 192-0392, Japan |
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| Abstract: | 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. |
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