Purine derivatives as potent γ-secretase modulators
- Author
- RIVKIN, Alexey1 ; AHEARN, Sean P1 ; OTTE, Karin M1 ; CHAOMIN LI1 ; ROSENAU, Andrew1 ; SURDI, Laura M1 ; JOON JUNG1 ; HUGHES, Bethany L1 ; CRISPINO, Jamie L1 ; NIKOV, George N1 ; MIDDLETON, Richard E1 ; MOXHAM, Christopher M1 ; CHICHETTI, Stephanie M1 ; SZEWCZAK, Alexander A; SHAH, Sanjiv2 ; MOY, Lily Y2 ; KENIFIC, Candia M2 ; TANGA, Flobert2 ; CRUZ, Jonathan C2 ; ANDRADE, Paula3 ; ANGAGAW, Minilik H3 ; SHOMER, Nirah H3 ; MILLER, Thomas; HAMBLETT, Christopher L1 ; MUNOZ, Benito; SHEARMAN, Mark S2 ; GARCIA, Yudith1 ; MARTINEZ, Michelle1 ; HUBBS, Jed L1 ; REUTERSHAN, Michael H1 ; DANIELS, Matthew H1 ; SILIPHAIVANH, Phieng1
[1] Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, United States
[2] Department of Neuroscience Drug Discovery, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, United States
[3] Department of Laboratory Animal Resources, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2010, Vol 20, Num 7, pp 2279-2282, 4 p ; ref : 12 ref
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Keyword (fr)
- Activité enzymatique Animal transgénique Antialzheimer Aspartic endopeptidases Composé bicyclique Cycle 6 chaînons Dérivé de la pipérazine Dérivé de la pipéridine Dérivé de la purine Dérivé de la pyrimidine Dérivé du benzène Hétérocycle azote In vitro In vivo Inhibition Modulation Protéine précurseur amyloïde Relation structure activité Souris Synthèse chimique Purine(6-[3-t-butyl-6-méthylanilino]-2-[3,3-diméthyl-4-(4-méthoxyphényl)pipérazino]-7-méthyl) Purine(6-[3-t-butyl-6-méthylanilino]-7-méthyl-2-[4-(4-méthylpyrimidin-6-yloxy)pipéridino]) γ Secretase Enzyme Hydrolases Mammalia Peptidases Rodentia Vertebrata
- Keyword (en)
- Enzymatic activity Transgenic animal Antialzheimer agent Aspartic endopeptidases Bicyclic compound Six membered ring Piperazine derivatives Piperidine derivatives Purine derivatives Pyrimidine derivatives Benzene derivatives Nitrogen heterocycle In vitro In vivo Inhibition Modulation Amyloid precursor protein Structure activity relation Mouse Chemical synthesis Enzyme Hydrolases Mammalia Peptidases Rodentia Vertebrata
- Keyword (es)
- Actividad enzimática Animal transgénico Antialzheimer Aspartic endopeptidases Compuesto bicíclico Ciclo 6 eslabones Piperazina derivado Piperidina derivado Purina derivado Pirimidina derivado Benceno derivado Heterociclo nitrógeno In vitro In vivo Inhibición Modulación Proteína precursor amiloide Relación estructura actividad Ratón Síntesis química Enzima Hydrolases Mammalia Peptidases Rodentia Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02B Neuropharmacology / 002B02B02 Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
- Francis
- 770 Psychology. Psychoanalysis. Psychiatry / 770-E Psychopharmacology / 770-E02 Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer…
- Discipline
- Pharmacological treatments Psychopathology. Psychiatry. Clinical psychology
- Origin
- Inist-CNRS
- Database
- FRANCIS ; PASCAL
- INIST identifier
- 22824898
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmcl.2010.02.008 
https://dx.doi.org/10.1016/j.bmcl.2010.02.008
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