Fluorine-Substitution in Cholesteryl Ester Transfer Protein Inhibitors (CETPInhibitors) – Biology, Chemistry, SAR, and Properties


  • Holger Paulsena
  • Siegfried Zaiss
  • Delf Schmidt
  • Hilmar Bischoff
  • Klaus-Dieter Bremm
  • Paul Naab
  • Michael Lögers
  • Stephan N. Wirtz
  • Jürgen Stoltefuss
  • Gunter Schmidt
  • Arndt Brandes
  • Carsten Schmeck
  • Stefan Antons




Cholesteryl ester transfer protein, Domino reaction, Hantzsch-reaction, Hdl-c elevation, Oxazaborolidine reduction


The inhibition of the cholesteryl ester transfer protein (CETP) provides a method for the elevation of the high density lipoprotein cholesterol (HDL-C) level, i.e. the 'good' cholesterol. The expected anti-atherogenic effect of this approach is independent of the proven benefits of lowering the low density lipoprotein cholesterol (LDL-C) level, i.e. the 'bad' cholesterol. A medicinal chemistry project is presented starting from the first screening hit to the second generation development candidate. The structure–activity relationship, the syntheses and the role of fluorine during optimization, as well as the biological activities are discussed.




How to Cite

H. Paulsena, S. Zaiss, D. Schmidt, H. Bischoff, K.-D. Bremm, P. Naab, M. Lögers, S. N. Wirtz, J. Stoltefuss, G. Schmidt, A. Brandes, C. Schmeck, S. Antons, Chimia 2004, 58, 123, DOI: 10.2533/000942904777678082.