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Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors

Cumming, J.N. ; Le, T.X. ; Babu, S. ; Carroll, C. ; Chen, X. ; Favreau, L. ; Gaspari, P. ; Guo, T. ; Hobbs, D.W. ; Huang, Y. ; Iserloh, U. ; Kennedy, M.E. ; Kuvelkar, R. ; Li, G. ; Lowrie, J. ; McHugh, N.A. ; Ozgur, L. ; Pan, J. ; Parker, E.M. ; Saionz, K. ; Stamford, A.W. ; Strickland, C. ; Tadesse, D. ; Voigt, J. ; Wang, L. ; Wu, Y. ; Zhang, L. ; Zhang, Q.

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3236-3241 [Periódico revisado por pares]

Oxford: Elsevier Ltd

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Título:
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
Autor: Cumming, J.N. ; Le, T.X. ; Babu, S. ; Carroll, C. ; Chen, X. ; Favreau, L. ; Gaspari, P. ; Guo, T. ; Hobbs, D.W. ; Huang, Y. ; Iserloh, U. ; Kennedy, M.E. ; Kuvelkar, R. ; Li, G. ; Lowrie, J. ; McHugh, N.A. ; Ozgur, L. ; Pan, J. ; Parker, E.M. ; Saionz, K. ; Stamford, A.W. ; Strickland, C. ; Tadesse, D. ; Voigt, J. ; Wang, L. ; Wu, Y. ; Zhang, L. ; Zhang, Q.
Assuntos: Alzheimer’s disease ; Amyloid Precursor Protein Secretases - antagonists & inhibitors ; Animals ; Aspartic Acid Endopeptidases - antagonists & inhibitors ; Aspartyl protease inhibitors ; BACE ; Biological and medical sciences ; Crystallography, X-Ray ; Disease Models, Animal ; Drug Design ; Humans ; Imidazolidines - chemical synthesis ; Imidazolidines - chemistry ; Imidazolidines - pharmacology ; Medical sciences ; Mice ; Mice, Transgenic ; Models, Molecular ; Molecular Conformation ; Molecular Structure ; Neuropharmacology ; Peptidomimetics ; Pharmacology. Drug treatments ; Piperazines - chemical synthesis ; Piperazines - chemistry ; Piperazines - pharmacology ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Structure-Activity Relationship ; β-Secretase
É parte de: Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3236-3241
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: Two novel, potent cyclic amine motifs for BACE1 inhibitors are described, along with their SAR in both the non-prime and prime subsites. Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2′ pocket.
Editor: Oxford: Elsevier Ltd
Idioma: Inglês

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Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors

Oxford: Elsevier Ltd

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