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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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