A novel class of sodium/calcium exchanger inhibitors: design, synthesis, and structure-activity relationships of 4-phenyl-3-(piperidin-4-yl)-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 Division, 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 of 3,4-dihydro-2(1H)-quinazolinone derivatives as sodium/calcium (Na+/Ca2+) exchanger inhibitors are described. In these studies, optimization of the substituents at the 3-position of this series of compounds was carried out and dramatic effects of the substituent on the activities were observed. Based on these SAR studies, a highly potent inhibitor of the Na+/Ca2+ exchanger, which showed single-digit-nanomolar activity, was discovered. |
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