Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (18), p.5380-5384
2010
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Details
- Autor(en) / Beteiligte
- Titel
- Iminoheterocycles as γ-secretase modulators
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (18), p.5380-5384
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The synthesis of a novel series of iminoheterocycles and their structure–activity relationship (SAR) as modulators of γ-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a structurally unique bicyclic core. Selected compounds exhibit good potency as γ-secretase modulators, excellent rat pharmacokinetics, and lowering of Aβ 42 levels in various in vivo models. The synthesis of a novel series of iminoheterocycles and their structure–activity relationship (SAR) as modulators of γ-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a structurally unique bicyclic core. Selected compounds exhibit good potency as γ-secretase modulators, excellent rat pharmacokinetics, and lowering of Aβ 42 levels in various in vivo models.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.07.121Titel-ID: cdi_proquest_miscellaneous_754011023
- Format
- –
- Schlagworte
- Alzheimer Disease - drug therapy, Alzheimer’s disease, Amyloid beta-Peptides - antagonists & inhibitors, Amyloid beta-Peptides - metabolism, Amyloid Precursor Protein Secretases - metabolism, Animals, Biological and medical sciences, Brain - metabolism, Bridged Bicyclo Compounds, Heterocyclic - chemistry, Bridged Bicyclo Compounds, Heterocyclic - pharmacokinetics, Bridged Bicyclo Compounds, Heterocyclic - therapeutic use, Humans, Imines - chemistry, Imines - pharmacokinetics, Imines - therapeutic use, Medical sciences, Mice, Mice, Transgenic, Neuropharmacology, Peptide Fragments - antagonists & inhibitors, Peptide Fragments - metabolism, Pharmacology. Drug treatments, 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 modulators