Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). Part 1: identification and structure-activity relationships of a novel series of substituted N-alkyl-N-biphenylylmethyl-N'-arylureas.

@article{Tanaka1998InhibitorsOA,
  title={Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). Part 1: identification and structure-activity relationships of a novel series of substituted N-alkyl-N-biphenylylmethyl-N'-arylureas.},
  author={Akito Tanaka and Takeshi Terasawa and Hiroji Hagihara and Yoko Sakuma and N Ishibe and Masae Sawada and Hisashi Takasugi and Hirokazu Tanaka},
  journal={Bioorganic & medicinal chemistry},
  year={1998},
  volume={6 1},
  pages={15-30}
}
A series of N-alkyl-N-biphenylylmethyl-N'-arylurea and related derivatives represented by 1 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Linking of two phenyl groups via oxygen and introduction of fluorine at appropriate positions on the biphenyl moiety improved in vitro and in vivo activity. From this series of analogs, compound 40 (FR179254), which had… CONTINUE READING

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