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
  • 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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