Synthesis of 3-ureido derivatives of coumarin and 2-quinolone as potent acyl-CoA: cholesterol acyltransferase inhibitors.

Chemical & pharmaceutical bulletin

PubMedID: 7600615

Tawada H, Natsugari H, Ishikawa E, Sugiyama Y, Ikeda H, Meguro K. Synthesis of 3-ureido derivatives of coumarin and 2-quinolone as potent acyl-CoA: cholesterol acyltransferase inhibitors. Chem Pharm Bull. 1995;43(4):616-25.
Novel 3-ureido derivatives of 4-phenylcoumarin and 4-phenyl-2-quinolone were synthesized and evaluated for acyl-CoA: cholesterol acyltransferase (ACAT)-inhibitory activity. These derivatives inhibited rat intestinal ACAT with IC50 values at the 10(-8) to 10(-9) M level and were found to normalize plasma cholesterol levels in cholesterol-fed rats when administered as dietary admixtures.