Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2279-2282
- Rivkin, Alexey
- Ahearn, Sean P.
- Chichetti, Stephanie M.
- Hamblett, Christopher L.
- Garcia, Yudith
- Martinez, Michelle
- Hubbs, Jed L.
- Reutershan, Michael H.
- Daniels, Matthew H.
- Siliphaivanh, Phieng
- Otte, Karin M.
- Li, Chaomin
- Rosenau, Andrew
- Surdi, Laura M.
- Jung, Joon
- Hughes, Bethany L.
- Crispino, Jamie L.
- Nikov, George N.
- Middleton, Richard E.
- Moxham, Christopher M.
- Szewczak, Alexander A.
- Shah, Sanjiv
- Moy, Lily Y.
- Kenific, Candia M.
- Tanga, Flobert
- Cruz, Jonathan C.
- Andrade, Paula
- Angagaw, Minilik H.
- Shomer, Nirah H.
- Miller, Thomas
- Munoz, Benito
- Shearman, Mark S.
2010
Volltextzugriff (PDF)
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- Autor(en) / Beteiligte
- Rivkin, Alexey
- Ahearn, Sean P.
- Chichetti, Stephanie M.
- Hamblett, Christopher L.
- Garcia, Yudith
- Martinez, Michelle
- Hubbs, Jed L.
- Reutershan, Michael H.
- Daniels, Matthew H.
- Siliphaivanh, Phieng
- Otte, Karin M.
- Li, Chaomin
- Rosenau, Andrew
- Surdi, Laura M.
- Jung, Joon
- Hughes, Bethany L.
- Crispino, Jamie L.
- Nikov, George N.
- Middleton, Richard E.
- Moxham, Christopher M.
- Szewczak, Alexander A.
- Shah, Sanjiv
- Moy, Lily Y.
- Kenific, Candia M.
- Tanga, Flobert
- Cruz, Jonathan C.
- Andrade, Paula
- Angagaw, Minilik H.
- Shomer, Nirah H.
- Miller, Thomas
- Munoz, Benito
- Shearman, Mark S.
- Titel
- Purine derivatives as potent γ-secretase modulators
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2010-04, Vol.20 (7), p.2279-2282
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- The development of a novel series of purines as γ-secretase modulators for potential use in the treatment of Alzheimer’s disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based γ-secretase modulators with 300- to 2000-fold in vitro selectivity over inhibition of Notch cleavage and that selectively reduces Αβ42 in an APP-YAC transgenic mouse model. The development of a novel series of purines as γ-secretase modulators for potential use in the treatment of Alzheimer’s disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based γ-secretase modulators with 300- to 2000-fold in vitro selectivity over inhibition of Notch cleavage and that selectively reduces Αβ42 in an APP-YAC transgenic mouse model.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2010.02.008Titel-ID: cdi_proquest_miscellaneous_733634378
- Format
- –
- Schlagworte
- Alzheimer Disease - drug therapy, Amyloid beta-Peptides - antagonists & inhibitors, Amyloid beta-Peptides - metabolism, Amyloid Precursor Protein Secretases - genetics, Amyloid Precursor Protein Secretases - metabolism, Animals, Biological and medical sciences, Humans, 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, Purines - chemistry, Purines - pharmacology, Purines - therapeutic use, Receptors, Notch - metabolism, Structure-Activity Relationship