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 pyrazole ring

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 1, 1998, Pages 81-86

  Tanaka, Akira ^a   Terasawa, Takeshi ^a   Hagihara, Hiroyuki ^a   Kinoshita, Takayoshi ^a   Sakuma, Yuri ^a   Ishibe, Noriko ^a   Sawada, Masae ^a   Takasugi, Hisashi ^a   Tanaka, Hirokazu ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLESTEROL; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; FR 186054; PYRAZOLE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BEAR; BIOAVAILABILITY; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG EFFICACY; DRUG SYNTHESIS; FEEDING; HYPERCHOLESTEROLEMIA; MOLECULAR MODEL; NONHUMAN; ORAL DRUG ADMINISTRATION; RABBIT;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; MOLECULAR STRUCTURE; PYRAZOLES; RABBITS; RATS; STEROL O-ACYLTRANSFERASE; UREA;

ANIMALIA; ORYCTOLAGUS CUNICULUS;

EID: 0032488587     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)10191-3     Document Type: Article

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26. w = 0.042.
27. 2: C, 63.78; H, 5.56; N, 14.30. Found: C, 63.94; H, 5.65; N, 14.20.
28. 2. The full paper will describe this optimization in greater detail.