Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubility |
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| Authors: | Ban Hitoshi Muraoka Masami Ioriya Katsuhisa Ohashi Naohito |
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| Affiliation: | Research Division, Sumitomo Pharmaceuticals Co., Ltd 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-0022, Japan. ban@sumitomopharm.co.jp |
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| Abstract: | 4-Aryl-1,8-naphthyridin-2(1H)-on-3-yl urea derivatives with hydrophilic groups were synthesized in order to improve aqueous solubility and pharmacokinetic property. SMP-797 possessing (4-aminophenyl)ureido and 3-(hydroxypropoxyphenyl) moieties showed potent ACAT inhibitory activity and excellent oral efficacy. |
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