2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 1998 Jan 6;8(1):81-6. doi: 10.1016/s0960-894x(97)10191-3.
A Tanaka 1,  T Terasawa,  H Hagihara,  T Kinoshita,  Y Sakuma,  N Ishibe,  M Sawada,  H Takasugi,  H Tanaka
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., Osaka, Japan.
PMID: 9871633 DOI: 10.1016/s0960-894x(97)10191-3
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 vitro efficacy, irrespective of dosing method, indicating superior characteristics compared to other ACAT inhibitors.

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