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

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...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2011/11/01, Vol.59(11), pp.1369-1375
Hauptverfasser:	Ogino, Masaki, Nakada, Yoshihisa, Negoro, Nobuyuki, Itokawa, Shigekazu, Nishimura, Satoshi, Sanada, Tsukasa, Satomi, Tomoko, Kita, Shunbun, Kubo, Kazuki, Marui, Shogo
Format:	Artikel
Sprache:	eng
Schlagworte:	(4-phenylcoumarin)acetanilide Acetanilides - chemical synthesis Acetanilides - chemistry Acetanilides - toxicity Acyl Coenzyme A - metabolism acyl-CoA: cholesterol acyltransferase inhibitor Administration, Oral Adrenal Cortex - drug effects adrenal toxicity Animals Anticholesteremic Agents - chemical synthesis Anticholesteremic Agents - chemistry Anticholesteremic Agents - toxicity atherosclerosis Carboxylic Acids - chemistry Cell Line cholesterol Coumarins - chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - toxicity Guinea Pigs Humans macrophage Models, Animal Rabbits Sterol O-Acyltransferase - antagonists & inhibitors Sterol O-Acyltransferase - metabolism
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