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2 results on '"cholesteryl ester transfer protein"'

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

Author

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, and Stefan Antons

Subjects
Cholesteryl ester transfer protein, Domino reaction, Hantzsch-reaction, Hdl-c elevation, Oxazaborolidine reduction, Chemistry, QD1-999
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.

Published
2004
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2. Fluorine-Substitution in Cholesteryl Ester Transfer Protein Inhibitors (CETPInhibitors) – Biology, Chemistry, SAR, and Properties

Author

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

Subjects
biology, Chemistry, Cholesterol, Oxazaborolidine reduction, Domino reaction, Low density lipoprotein cholesterol, chemistry.chemical_element, Hantzsch-reaction, General Medicine, General Chemistry, Cholesteryl ester transfer protein, chemistry.chemical_compound, High-density lipoprotein, Biochemistry, Cholesterylester transfer protein, Fluorine, biology.protein, lipids (amino acids, peptides, and proteins), Hdl-c elevation, QD1-999
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.

Published
2004

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