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香豆素和2-喹诺酮的3-脲基衍生物作为强效酰基辅酶A：胆固醇酰基转移酶抑制剂的合成。

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

作者信息

Tawada H, Natsugari H, Ishikawa E, Sugiyama Y, Ikeda H, Meguro K

机构信息

Pharmaceutical Research Laboratories II, Takeda Chemical Industries, Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1995 Apr;43(4):616-25. doi: 10.1248/cpb.43.616.

DOI:10.1248/cpb.43.616
PMID:7600615
Abstract

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.

摘要

合成了新型的4-苯基香豆素和4-苯基-2-喹诺酮的3-脲基衍生物，并对其酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制活性进行了评估。这些衍生物以10（-8）至10（-9）M的IC50值抑制大鼠肠道ACAT，并且当作为膳食添加剂给药时，发现其可使胆固醇喂养大鼠的血浆胆固醇水平正常化。

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