Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA: cholesterol O-acyltransferase (ACAT) bearing …

A Tanaka, T Terasawa, H Hagihara, T Kinoshita…

Index: Tanaka, Akira; Terasawa, Takeshi; Hagihara, Hiroyuki; Kinoshita, Takayoshi; Sakuma, Yuri; Ishibe, Noriko; Sawada, Masae; Takasugi, Hisashi; Tanaka, Hirokazu Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 1 p. 81 - 86

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Citation Number: 14

Abstract

The synthesis, single crystal X-ray structural analysis, and biological activity of FR186054 (2c), a new, potent, orally efficacious inhibitor of acyl-CoA: cholesterol O-acyltransferase (ACAT), containing a pyrazole ring are described. This compound displayed excellent in vivo efficacy, irrespective of dosing method, indicating superior characteristics compared to other ACAT inhibitors.