Synthesis of 3-ureido derivatives of coumarin and 2-quinolone as potent Acyl-CoA: Cholesterol acyltransferase inhibitors

DOI: 10.1248/cpb.43.616

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 616 - 625 (1995)

Update date:2022-08-04

Topics:

Authors:

Tawada Tawada

Natsugari

Ishikawa

Sugiyama

Ikeda Ikeda

Meguro Meguro

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Article abstract of DOI:10.1248/cpb.43.616

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.

Full text of DOI:10.1248/cpb.43.616

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