Open AccessFluorine-Substitution in Cholesteryl Ester Transfer Protein Inhibitors (CETPInhibitors) – Biology, Chemistry, SAR, and Properties
Author(s) -
Holger Paulsena,
Carsten Schmeck,
Arndt Brandes,
Günter Schmidt,
J. Stoltefuß,
Stephan N. Wirtz,
Michael Lögers,
Paul Naab,
K D Bremm,
Hilmar Bischoff,
Delf Schmidt,
S. Zaiss,
Stephanie Antons
Publication year - 2004
Publication title -
chimia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.387
H-Index - 55
eISSN - 2673-2424
pISSN - 0009-4293
DOI - 10.2533/000942904777678082
Subject(s) - cholesterylester transfer protein , cholesterol , chemistry , cholesteryl ester , fluorine , lipoprotein , high density lipoprotein , biochemistry , organic chemistry
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.