2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2640-4. doi: 10.1016/j.bmcl.2008.03.030. Epub 2008 Mar 14.

Abstract

2-Arylbenzoxazole 5 was identified as a hit from a fluorescence-based high-throughput screen for CETP inhibitors. The synthesis and SAR investigation employing array synthesis of the A- and B-rings are described.

MeSH terms

  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / chemistry
  • Benzoxazoles / pharmacology*
  • Cholesterol Ester Transfer Proteins / antagonists & inhibitors*
  • Cholesterol Ester Transfer Proteins / metabolism
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Benzoxazoles
  • Cholesterol Ester Transfer Proteins