391687-64-2Relevant academic research and scientific papers
Discovery of a novel acyl-CoA: Cholesterol acyltransferase inhibitor: The synthesis, biological evaluation, and reduced adrenal toxicity of (4-phenylcoumarin)acetanilide derivatives with a carboxylic acid moiety
Ogino, Masaki,Nakada, Yoshihisa,Negoro, Nobuyuki,Itokawa, Shigekazu,Nishimura, Satoshi,Sanada, Tsukasa,Satomi, Tomoko,Kita, Shunbun,Kubo, Kazuki,Marui, Shogo
, p. 1369 - 1375 (2012/01/02)
As a part of our research for novel potent and orally available acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors that can be used as anti-atherosclerotic agents, we recently reported the discovery of the (4-phenylcoumarine) acetanilide derivative 1. However, compound 1 showed adrenal toxicity in animal models. In order to search for safer ACAT inhibitors that do not have adrenal toxicity, we examined the inhibitory activity of ACAT in human macrophage and adrenal cells. The introduction of a carboxylic acid moiety on the pendant phenyl ring and the adjustment of the lipophilicity led to the discovery of (2E)-3-[7-chloro-3-[2-[[4-fluoro-2-(trifluoromethyl) phenyl]amino]-2-oxoethyl]-6-methyl-2-oxo-2H-chromen-4-yl]phenyl]acrylic acid (21e), which showed potent ACAT inhibitory activity in macrophages and a selectivity of around 30-fold over adrenal cells. In addition, compound 21e showed high adrenal safety in guinea pigs.
COUMARIN DERIVATIVE AND USE THEREOF
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Page/Page column 73-75, (2008/06/13)
The present invention relates to an alkaline earth metal salt or an organic amine salt of a compound represented by the formula [I]: wherein R1 and R2 are each a hydrogen atom, a halogen atom, or an optionally substituted linear hydrocarbon group; ring A is an optionally further substituted benzene ring; B is an optionally substituted benzene ring; R is a carboxyl group or a linear hydrocarbon group substituted with a carboxyl group and the like.
COUMARIN DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND USE THEREOF
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Page 38; 39, (2010/02/08)
Compounds represented by the general formula [I]: wherein R1 and R2 are each hydrogen, halogen, an optionally substituted linear hydrocarbon group, or hydroxyl which may be substituted with an optionally substituted liner hydrocarbon
Lipid-rich plaque inhibitors
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Page 70, (2010/02/06)
The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is —NR1— (in which
