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

Authors

  • 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

DOI:

https://doi.org/10.2533/000942904777678082

Keywords:

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

Abstract

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.

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Published

2004-03-01

Issue

Vol. 58 No. 3 (2004): Fluorine in the Life Science Industry

Section

Scientific Articles

License

Copyright (c) 2004 Swiss Chemical Society

Creative Commons License

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

How to Cite

[1]
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.