Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors

Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (8), p.2554-2558
Hauptverfasser:	Griebenow, Nils, Flessner, Timo, Buchmueller, Anja, Raabe, Martin, Bischoff, Hilmar, Kolkhof, Peter
Format:	Artikel
Sprache:	eng
Schlagworte:	alkyl (aryl) transferases Animals Benzazepines - chemical synthesis Benzazepines - chemistry Benzazepines - pharmacokinetics Biological and medical sciences Crystallography, X-Ray enzyme inhibitors Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Farnesyl-Diphosphate Farnesyltransferase - antagonists & inhibitors Farnesyl-Diphosphate Farnesyltransferase - metabolism General and cellular metabolism. Vitamins heterocyclic compounds Humans Medical sciences Mice Microsomes, Liver - metabolism Molecular Conformation Pharmacology. Drug treatments Stereoisomerism Structure-Activity Relationship structure-activity relationships
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Beschreibung
Zusammenfassung:	Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.02.004