Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: novel, highly potent and orally efficacious squalene synthase inhibitors.

@article{Ichikawa2011DiscoveryOA,
  title={Discovery of atrop fixed alkoxy-aminobenzhydrol derivatives: novel, highly potent and orally efficacious squalene synthase inhibitors.},
  author={Masanori Ichikawa and A. Yokomizo and M. Itoh and Noriyasu Haginoya and K. Sugita and H. Usui and K. Terayama and Akira Kanda},
  journal={Bioorganic & medicinal chemistry},
  year={2011},
  volume={19 17},
  pages={
          5207-24
        }
}
We have recently reported the discovery of the new benzhydrol template, which has a highly potent inhibitory activity for squalene synthase, as typified by compound 1 (SSI IC(50)=0.85 nM). However, it was composed of a pair of easy rotatable atropisomers. In the effort to fix the isomerization, a highly potent alkoxy-aminobenzhydrol scaffold was developed. Some of these acquired compounds demonstrating strong cholesterol synthesis inhibitory activities in a rat hepatic cell. Moreover, two of… Expand
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