Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein inhibitors

Molecules. 2010 Aug 19;15(8):5721-33. doi: 10.3390/molecules15085721.

Abstract

Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previously-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzoxazines / chemical synthesis*
  • Benzoxazines / chemistry
  • Benzoxazines / pharmacology*
  • Benzyl Compounds / chemical synthesis*
  • Benzyl Compounds / chemistry
  • Benzyl Compounds / pharmacology*
  • Cholesterol Ester Transfer Proteins / antagonists & inhibitors*
  • Models, Molecular
  • Quantitative Structure-Activity Relationship
  • Rabbits

Substances

  • Benzoxazines
  • Benzyl Compounds
  • Cholesterol Ester Transfer Proteins