Synthesis and structure-activity relationship studies on a novel series of naphthylidinoylureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) |
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Authors: | Ohnuma Satoshi Muraoka Masami Ioriya Katsuhisa Ohashi Naohito |
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Institution: | Research Division, Sumitomo Pharmaceuticals Co. Ltd, 1-98 Kasugade Naka 3-chome, Konohana-ku, Osaka 554-0022, Japan. ohnuma@sumitomopharm.co.jp |
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Abstract: | The synthesis and structure-activity relationships of N-phenyl-N'-3-(4-phenylnaphthylidinoyl)]urea derivatives 3 as a novel structural class of potent ACAT inhibitors is described. A 3-methoxy group substituted on the naphthylidinone 4-phenyl ring, together with a 1-N-(n)butyl substitution, SM-32504 (3m), gave a potent ACAT inhibitor, in vitro, respectively. The most potent compound, SM-32504 (3m), decreased the serum cholesterol level significantly in a high fat and high cholesterol-fed mouse model. |
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