Fluorinated piperidine acetic acids as γ-secretase modulators (original) (raw)
A Substrate-Based Difluoro Ketone Selectively Inhibits Alzheimer's γ-Secretase Activity
Michael Wolfe
Journal of Medicinal Chemistry, 1998
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Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach
Tina Talreja
Bioorganic & Medicinal Chemistry Letters, 2011
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Lead optimization of 4,4-biaryl piperidine amides as γ-secretase inhibitors
Lina Xu, Flobert Tanga
Bioorganic & Medicinal Chemistry Letters, 2012
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Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
Ricardo Lira
Bioorganic & Medicinal Chemistry Letters, 2012
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1-Amino-4,4-difluorocyclohexanecarboxylic acid as a promising building block for drug discovery: Design, synthesis and characterization
Pavel Mykhailiuk
2013
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Synthesis of Pyridopyrazine-1,6-dione γ-Secretase Modulators via Selective 4-Methylimidazole N1-Buchwald Arylation
Neal Sach
The Journal of Organic Chemistry, 2019
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Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors
Amin Nomeir
Bioorganic & Medicinal Chemistry Letters, 2007
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Purine derivatives as potent γ-secretase modulators
Yudith Garcia
Bioorganic & Medicinal Chemistry Letters, 2010
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N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase
Gary Probst
Bioorganic & Medicinal Chemistry Letters, 2009
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Pyridine-derived γ-secretase modulators
Adrian Hall
Bioorganic & Medicinal Chemistry Letters, 2011
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N-{N-[2-(3,5-Difluorophenyl)acetyl]-(S)-alanyl}-(S)-phenylglycinetert-butyl ester (DAPT): an inhibitor of γ-secretase, revealing fine electronic and hydrogen-bonding features
Francisco Valenzuela
Acta Crystallographica Section C Crystal Structure Communications, 2010
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II)
Martin Neitzel, Elizabeth Brigham, Jacek Jagodzinski
Bioorganic & Medicinal Chemistry Letters, 2010
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1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic Acid (CHF5074), a Novel -Secretase Modulator, Reduces Brain beta-Amyloid Pathology in a Transgenic Mouse Model of Alzheimer's Disease without Causing Peripheral Toxicity
Vladimiro Pietrini
Journal of Pharmacology and Experimental Therapeutics, 2007
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Discovery and initial optimization of 5,5′-disubstituted aminohydantoins as potent β-secretase (BACE1) inhibitors
Kristi Fan, Ann Aulabaugh
Bioorganic & Medicinal Chemistry Letters, 2010
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New 4-Aminopyridine derivatives containing peptide fragment designed for the treatment of Alzheimer disease and multiple sclerosis
Borislav Anchev
Proceedings of the 35th European Peptide Symposium
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Development of Fluorine-18-Labeled 5-HT1A Antagonists
Lixin Lang
Journal of Medicinal Chemistry, 1999
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Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability
Amin Nomeir
Bioorganic & Medicinal Chemistry Letters, 2009
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(S)-N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor
Anthony Kreft
Bioorganic & Medicinal Chemistry Letters, 2009
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Author's personal copy Practical syntheses of 4-fluoroprolines
Mukund Chorghade
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Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): A γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer’s disease
Suresh Yeola
Bioorganic & Medicinal Chemistry Letters, 2007
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1-(3′, 4′-Dichloro-2-fluoro [1, 1′-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel γ-secretase modulator, reduces brain β-amyloid pathology in a …
B. Imbimbo
… of Pharmacology and …, 2007
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Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease
Santosh Prajapati
European Journal of Medicinal Chemistry, 2019
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