Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors

This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (11), p.3671-3675
Hauptverfasser:	Escribano, Ana, Mateo, Ana I., Martin de la Nava, Eva M., Mayhugh, Daniel R., Cockerham, Sandra L., Beyer, Thomas P., Schmidt, Robert J., Cao, Guoqing, Zhang, Youyan, Jones, Timothy M., Borel, Anthony G., Sweetana, Stephanie A., Cannady, Ellen A., Mantlo, Nathan B.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apolipoprotein A-I - genetics Apolipoprotein A-I - metabolism Biological and medical sciences CETP inhibitor chemistry Cholesterol Ester Transfer Proteins - antagonists & inhibitors Cholesterol Ester Transfer Proteins - genetics Cholesterol Ester Transfer Proteins - metabolism Cholesterol, HDL - drug effects Cholesterol, HDL - metabolism Dogs Drug Design Female genetically modified organisms HDL-c Hypolipidemic Agents - chemical synthesis Hypolipidemic Agents - chemistry Hypolipidemic Agents - pharmacokinetics Injections, Intravenous Male Medical sciences Mice Mice, Transgenic Pharmacokinetics Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - chemistry Quinolines - pharmacokinetics Rats Rats, Sprague-Dawley Structure-Activity Relationship Tetrahydroquinolines Tetrazoles - chemical synthesis Tetrazoles - chemistry Tetrazoles - pharmacokinetics
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Beschreibung
Zusammenfassung:	This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.04.042