Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
- Author
- GUMMING, J. N1 ; LE, T. X1 2 ; ISERLOH, U1 ; KENNEDY, M. E1 ; KUVELKAR, R1 ; LI, G1 ; LOWRIE, J1 2 ; MCHUGH, N. A1 ; OZGUR, L1 2 ; PAN, J1 ; PARKER, E. M1 ; SAIONZ, K1 2 ; BABU, S1 2 ; STAMFORD, A. W3 ; STRICKLAND, C3 ; TADESSE, D2 3 ; VOIGT, J3 ; WANG, L3 ; WU, Y3 ; ZHANG, L3 ; ZHANG, Q3 ; CARROLL, C1 2 ; CHEN, X1 ; FAVREAU, L1 ; GASPARI, P1 2 ; GUO, T1 2 ; HOBBS, D. W1 2 ; HUANG, Y1
[1] Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States
[2] Pharmacopeia, Inc., PO BOX 5350, Princeton, NJ 08543, United States
[3] Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2008, Vol 18, Num 11, pp 3236-3241, 6 p
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Oxford
- Publication country
- United Kingdom
- Document type
- Article
- Language
- English
- Author keyword
- Alzheimer's disease Aspartyl protease inhibitors BACE Peptidomimetics β-Secretase
- Keyword (fr)
- Animal Antialzheimer Aspartic endopeptidases Carboxamide Complexe enzyme inhibiteur Composé peptidomimétique Diffraction RX Démence d'Alzheimer Dérivé de l'imidazole Dérivé de la pipérazine In vitro In vivo Inhibiteur enzyme Inhibiteur protease Protéine précurseur amyloïde Relation structure activité Souris Structure cristalline Structure moléculaire Synthèse chimique β-secretase Imidazolidine dérivé Imidazolidinone dérivé Inhibiteur BACE1 Isophtalamide dérivé Memapsin 2 Pipérazinone dérivé Enzyme Hydrolases Maladie dégénérative Mammalia Pathologie de l'encéphale Pathologie du système nerveux central Pathologie du système nerveux Peptidases Rodentia Vertebrata
- Keyword (en)
- Animal Antialzheimer agent Aspartic endopeptidases Carboxamide Inhibitor enzyme complex Peptidomimetic compound X ray diffraction Alzheimer disease Imidazole derivatives Piperazine derivatives In vitro In vivo Enzyme inhibitor Protease inhibitor Amyloid precursor protein Structure activity relation Mouse Crystalline structure Molecular structure Chemical synthesis β-secretase Enzyme Hydrolases Degenerative disease Mammalia Cerebral disorder Central nervous system disease Nervous system diseases Peptidases Rodentia Vertebrata
- Keyword (es)
- Animal Antialzheimer Aspartic endopeptidases Carboxamida Complejo enzima inhibidor Compuesto peptidomimético Difracción RX Demencia Alzheimer Imidazol derivado Piperazina derivado In vitro In vivo Inhibidor enzima Inhibidor proteasa Proteína precursor amiloide Relación estructura actividad Ratón Estructura cristalina Estructura molecular Síntesis química β-secretase Enzima Hydrolases Enfermedad degenerativa Mammalia Encéfalo patología Sistema nervosio central patología Sistema nervioso patología 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
- 20411652
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.2008.04.050 
https://dx.doi.org/10.1016/j.bmcl.2008.04.050
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