4-phenylcoumarin and Atherosclerosis

4-phenylcoumarin has been researched along with Atherosclerosis* in 1 studies

Other Studies

1 other study(ies) available for 4-phenylcoumarin and Atherosclerosis

Article	Year
Discovery of a potent and orally available acyl-CoA: cholesterol acyltransferase inhibitor as an anti-atherosclerotic agent: (4-phenylcoumarin)acetanilide derivatives. Chemical & pharmaceutical bulletin, 2011, Volume: 59, Issue:10 Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4-phenylcoumarin)acetanilide scaffold was identified. Evaluation of the structure-activity relationships of a substituent on this scaffold, with an emphasis on improving the pharmacokinetic profile led to the discovery of 2-[7-chloro-4-(3-chlorophenyl)-6-methyl-2-oxo-2H-chromen-3-yl]-N-[4-chloro-2-(trifluoromethyl)phenyl]acetamide (23), which exhibited potent ACAT inhibitory activity (IC50=12 nM) and good pharmacokinetic profile in mice. Compound 23 also showed regressive effects on atherosclerotic plaques in apolipoprotein (apo)E knock out (KO) mice at a dose of 0.3 mg/kg per os (p.o.). Topics: Acetamides; Acetanilides; Acyl Coenzyme A; Administration, Oral; Animals; Anticholesteremic Agents; Apolipoproteins; Atherosclerosis; Benzopyrans; Cholesterol; Coumarins; Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Enzyme Inhibitors; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Targeted Therapy; Structure-Activity Relationship	2011

Article

Year

Discovery of a potent and orally available acyl-CoA: cholesterol acyltransferase inhibitor as an anti-atherosclerotic agent: (4-phenylcoumarin)acetanilide derivatives.

Chemical & pharmaceutical bulletin, 2011, Volume: 59, Issue:10

Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4-phenylcoumarin)acetanilide scaffold was identified. Evaluation of the structure-activity relationships of a substituent on this scaffold, with an emphasis on improving the pharmacokinetic profile led to the discovery of 2-[7-chloro-4-(3-chlorophenyl)-6-methyl-2-oxo-2H-chromen-3-yl]-N-[4-chloro-2-(trifluoromethyl)phenyl]acetamide (23), which exhibited potent ACAT inhibitory activity (IC50=12 nM) and good pharmacokinetic profile in mice. Compound 23 also showed regressive effects on atherosclerotic plaques in apolipoprotein (apo)E knock out (KO) mice at a dose of 0.3 mg/kg per os (p.o.).

Topics: Acetamides; Acetanilides; Acyl Coenzyme A; Administration, Oral; Animals; Anticholesteremic Agents; Apolipoproteins; Atherosclerosis; Benzopyrans; Cholesterol; Coumarins; Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Enzyme Inhibitors; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Targeted Therapy; Structure-Activity Relationship

2011