2-Azetidinone cholesterol absorption inhibitors: Increased potency by substitution of the C-4 phenyl ring

Bioorganic and Medicinal Chemistry

Volumn 6, Issue 9, 1998, Pages 1429-1437

  Vaccaro, Wayne D ^a   Sher, Rosy ^a   Davis Jr , Harry R ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AZETIDINONE DERIVATIVE; HYPOCHOLESTEROLEMIC AGENT;

ANIMAL EXPERIMENT; ARTICLE; CHEMICAL MODIFICATION; CHOLESTEROL BLOOD LEVEL; DRUG POTENCY; DRUG SYNTHESIS; HAMSTER; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTICHOLESTEREMIC AGENTS; AZETIDINES; CHOLESTEROL; CRICETINAE; LIVER; MAGNETIC RESONANCE SPECTROSCOPY; MASS SPECTROMETRY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032169758     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0968-0896(98)00073-X     Document Type: Article

References (16)

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8. (b) Best yields were obtained when the imines were recrystallized prior to use in the ketene-imine reaction.
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10. ® AS column.
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15. Measured by reduction in liver cholesterol ester levels (L/CE) in the 7-day cholesterol fed hamster model. All compounds with indicated percent reductions were statistically different from the cholesterol-fed control group. The compounds were evaluated in a series of separate 7-day cholesterol-fed hamster studies hence, direct statistical comparisons among the compounds were not performed. See ref. 1 .
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