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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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
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container_end_page 2558
container_issue 8
container_start_page 2554
container_title Bioorganic & medicinal chemistry letters
container_volume 21
creator Griebenow, Nils
Flessner, Timo
Buchmueller, Anja
Raabe, Martin
Bischoff, Hilmar
Kolkhof, Peter
description Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.
doi_str_mv 10.1016/j.bmcl.2011.02.004
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source MEDLINE; Access via ScienceDirect (Elsevier)
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
title Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors
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