Discovery of a potent and orally available acyl-CoA: cholesterol acyltransferase inhibitor as an anti-atherosclerotic agent:(4-phenylcoumarin) acetanilide derivatives

…, R Tokunoh, S Itokawa, Y Kakoi, S Nishimura…

文献索引：Ogino, Masaki; Fukui, Seiji; Nakada, Yoshihisa; Tokunoh, Ryosuke; Itokawa, Shigekazu; Kakoi, Yuichi; Nishimura, Satoshi; Sanada, Tsukasa; Fuse, Hiromitsu; Kubo, Kazuki; Wada, Takeo; Marui, Shogo Chemical and Pharmaceutical Bulletin, 2011 , vol. 59, # 10 p. 1268 - 1273

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被引用次数: 10

摘要

Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4- phenylcoumarin) acetanilide scaffold was identified. Evaluation of the structure–activity relationships of a substituent on this scaffold, with an emphasis on improving the ...