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.
合成了4-苯基
香豆素和4-苯基-2-
喹诺酮的新型3-
脲基衍
生物,并评估了其酰基
辅酶A:
胆固醇酰基转移酶(ACAT)的抑制活性。这些衍
生物以10(-8)至10(-9)M的
水平抑制大鼠肠道ACAT的IC50值,并发现当以膳食混合物的形式给予
胆固醇喂养的大鼠时,血浆中的
胆固醇水平正常化。