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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-04, Vol.21 (8), p.2554-2558
Main Authors: Griebenow, Nils, Flessner, Timo, Buchmueller, Anja, Raabe, Martin, Bischoff, Hilmar, Kolkhof, Peter
Format: Article
Language:English
Subjects:
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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Description
Summary: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