Discovery of a novel potent Na+/Ca2+ exchanger inhibitor: design, synthesis and structure-activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives |
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Authors: | Hasegawa Hirohiko Muraoka Masami Matsui Kazuki Kojima Atsuyuki |
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Institution: | Research Center, Sumitomo Pharmaceuticals Co., Ltd., 1-98, Kasugadenaka 3-Chome, Konohana-ku, Osaka 554-0022, Japan. hhasegaw@sumitomopharm.co.jp |
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Abstract: | Design, synthesis and structure-activity relationships for 3,4-dihydro-2(1H)-quinazolinone derivatives with the inhibitory activities of the Na(+)/Ca(2+) exchanger are discussed. These studies based on lead compound 1a lead to the discovery of a structurally novel and highly potent inhibitor against the Na(+)/Ca(2+) exchanger 4f (SM-15811), which directly inhibited the Na(+)-dependent Ca(2+) influx via the Na(+)/Ca(2+) exchanger in cardiomyocytes with a high potency. |
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