Bioorganic & medicinal chemistry, 2008-01, Vol.18 (1), p.215-219
2008
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry, 2008-01, Vol.18 (1), p.215-219
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2008
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The design of amide and heteroaryl amide isosteres as replacements for the carbamate substructure in previously disclosed 2,6-disubstituted piperidine N-arylsulfonamides is described. In several cases, amides lessened CYP liabilities in this class of γ-secretase inhibitors. Selected compounds showed significant reduction of Aβ levels upon oral dosing in a transgenic murine model of Alzheimer’s disease.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894X, 0968-0896eISSN: 1464-3405, 1464-3391DOI: 10.1016/j.bmcl.2007.10.092Titel-ID: cdi_proquest_miscellaneous_70192316
- Format
- –
- Schlagworte
- Alzheimer’s disease, Amides - chemistry, Amides - pharmacokinetics, Amides - pharmacology, Amyloid beta-Peptides - metabolism, Amyloid Precursor Protein Secretases - antagonists & inhibitors, Animals, Biological and medical sciences, Carbamates - chemistry, Carbamates - pharmacokinetics, Carbamates - pharmacology, Cytochrome P-450 Enzyme Inhibitors, Heterocyclic Compounds - chemistry, Heterocyclic Compounds - pharmacokinetics, Heterocyclic Compounds - pharmacology, Medical sciences, Mice, Neuropharmacology, Oxadiazoles - chemistry, Oxadiazoles - pharmacokinetics, Oxadiazoles - pharmacology, Pharmacology. Drug treatments, Piperidines - chemistry, Piperidines - pharmacokinetics, Piperidines - pharmacology, Protease Inhibitors - chemistry, Protease Inhibitors - pharmacokinetics, Protease Inhibitors - pharmacology, Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer, Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease), Psychology. Psychoanalysis. Psychiatry, Psychopharmacology, Rats, Structure-Activity Relationship, γ-Secretase