Bioorganic & Medicinal Chemistry 2011-09-01

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

Masanori Ichikawa, Aki Yokomizo, Masao Itoh, Noriyasu Haginoya, Kazuyuki Sugita, Hiroyuki Usui, Koji Terayama, Akira Kanda

Index: Bioorg. Med. Chem. 19(17) , 5207-24, (2011)

Full Text: HTML

Abstract

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 the series compounds exhibited specific plasma lipid-lowering effects in in vivo animal models.Copyright © 2011 Elsevier Ltd. All rights reserved.

Related Compounds

  • Benzhydrol

Related Articles:

Semi-quantitative profile of regioisomeric monohydroxydiphenylmethane metabolites in rat urine, faeces and bile.

1981-06-01

[Xenobiotica 11(6) , 425-32, (1981)]

Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.

2011-03-15

[Bioorg. Med. Chem. 19 , 1930-1949, (2011)]

Calorimetric study of glass transition in molecular liquids consisting of globular associates: dicyclorohexylmethanol and tricyclohexylmethanol.

2012-04-05

[J. Phys. Chem. B 116(13) , 3938-43, (2012)]

Discovery of novel tricyclic compounds as squalene synthase inhibitors.

2012-05-01

[Bioorg. Med. Chem. 20(9) , 3072-93, (2012)]

[Determination of dimedrol and benzhydrol in the urine by high efficient liquid chromatographic method].

1980-01-01

[Sud. Med. Ekspert. 23(2) , 40-2, (1980)]

More Articles...