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.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Crystallography, X-Ray
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Molecular Structure
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology
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Rabbits
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Rats
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / chemistry
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Urea / pharmacology
Substances
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Enzyme Inhibitors
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Pyrazoles
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Urea
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FR 186054
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Sterol O-Acyltransferase