Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors
- Author
- HONG ZHU1 ; YOUNG, Mary B1 ; TUGUSHEVA, Katherine2 ; HOLAHAN, Marie A3 ; MICHENER, Maria S3 ; COOK, Jacquelynn J3 ; SIMON, Adam2 ; HAZUDA, Daria J2 ; VACCA, Joseph P1 ; RAJAPAKSE, Hemaka A1 ; NANTERMET, Philippe G1 ; GRAHAM, Samuel L1 ; COLUSSI, Dennis2 ; LAI, Ming-Tain2 ; PIETRAK, Beth2 ; PRICE, Eric A2 ; SANKARANARAYANAN, Sethu2 ; SHI, Xiao-Ping2
[1] Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, United States
[2] Department of Alzheimer's Research, Merck Research Laboratories, West Point, PA 19486, United States
[3] Department of Imaging Research, Merck Research Laboratories, West Point, PA 19486, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2010, Vol 20, Num 5, pp 1779-1782, 4 p ; ref : 15 ref
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- AD BACE Tertiary carbinamine
- Keyword (fr)
- Animal Antialzheimer Aspartic endopeptidases Barrière hématoencéphalique Chlore Composé organique Composé benzénique Démence d'Alzheimer Dérivé de la pyridine Dérivé du cyclopropane Fluor Composé organique In vitro In vivo Inhibiteur enzyme Protéine précurseur amyloïde Relation structure activité Singe Sulfonamide Synthèse chimique β-secretase 1,3,4-Oxadiazole dérivé Inhibiteur BACE Pyridine(4-[5-(α-amino-4-fluoro-α-méthylphénéthyl)-1,3,4-oxadiazol-2-yl]-3-chloro-2-[mésyl méthyl amino]-6-[2-méthoxyéthyl méthylcyclopropyl amino]) Enzyme Hydrolases Mammalia Peptidases Primates Vertebrata
- Keyword (en)
- Animal Antialzheimer agent Aspartic endopeptidases Blood brain barrier Chlorine Organic compounds Benzenic compound Alzheimer disease Pyridine derivatives Cyclopropane derivatives Fluorine Organic compounds In vitro In vivo Enzyme inhibitor Amyloid precursor protein Structure activity relation Monkey Sulfonamide Chemical synthesis β-secretase Enzyme Hydrolases Mammalia Peptidases Primates Vertebrata
- Keyword (es)
- Animal Antialzheimer Aspartic endopeptidases Barrera hematoencefálica Cloro Compuesto orgánico Compuesto bencénico Demencia Alzheimer Piridina derivado Ciclopropano derivado Fluor Compuesto orgánico In vitro In vivo Inhibidor enzima Proteína precursor amiloide Relación estructura actividad Mono Sulfonamida Síntesis química β-secretase Enzima Hydrolases Mammalia Peptidases Primates 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
- 22824793
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.2010.01.005 
https://dx.doi.org/10.1016/j.bmcl.2010.01.005
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