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AGING-US (2011)
Investigation of alpha-phenylnorstatine and alpha-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors
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Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
β-Secretase (BACE-1) inhibitory effect of biflavonoids
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
P2′-truncated BACE-1 inhibitors with a novel hydroxethylene-like core
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2010)
Design and Synthesis of Potent and Selective BACE-1 Inhibitors
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Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human β-Secretase (BACE1) Inhibitors
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JOURNAL OF MEDICINAL CHEMISTRY (2010)
A Noncompetitive BACE1 Inhibitor TAK-070 Ameliorates Aβ Pathology and Behavioral Deficits in a Mouse Model of Alzheimer's Disease
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Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and β-secretase
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BIOORGANIC & MEDICINAL CHEMISTRY (2009)
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Design and synthesis of cell potent BACE-1 inhibitors: Structure-activity relationship of P1′ substituents
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening
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Evolution of Tertiary Carbinamine BACE-1 Inhibitors: A beta Reduction in Rhesus CSF upon Oral Dosing
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Aminoimidazoles as Potent and Selective Human β-Secretase (BACE1) Inhibitors
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JOURNAL OF MEDICINAL CHEMISTRY (2009)
First Demonstration of Cerebrospinal Fluid and Plasma A beta Lowering with Oral Administration of a beta-Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates
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Acylguanidine inhibitors of β-secretase:: Optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor
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Acylguanidine inhibitors of β-secretase:: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)
α-Naphthylaminopropan-2-ol Derivatives as BACE1 Inhibitors
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γ-secretase inhibition and modulation for Alzheimer's disease
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Second generation of hydroxyethylamine BACE-1 inhibitors: Optimizing potency and oral bioavailability
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JOURNAL OF MEDICINAL CHEMISTRY (2008)
β-secretase as a therapeutic target for Alzheimer's disease
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In vivo β-Secretase 1 inhibition leads to brain Aβ lowering and increased α-secretase processing of amyloid precursor protein without effect on neuregulin-1
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JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2008)
2-amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme):: Use of structure based design to convert a micromolar hit into a nanomolar lead
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
Discovery of isonicotinamide derived β-secretase inhibitors:: In vivo reduction of β-amyloid
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)
Design, synthesis, and X-ray structure of potent memapsin 2 (β-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human β-secretase
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JOURNAL OF MEDICINAL CHEMISTRY (2007)
Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases β-cleavage of amyloid precursor protein and amyloid-β production in vivo
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JOURNAL OF NEUROCHEMISTRY (2007)
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ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2007)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)
Design of potent inhibitors of human beta-secretase. Part 2
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2007)
Discovery of oxadiazoyl tertiary carbinamine inhibitors of β-secretase (BACE-1)
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice
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JOURNAL OF NEUROCHEMISTRY (2006)
Acylguanidines as small-molecule β-secretase inhibitors
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
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JOURNAL OF MEDICINAL CHEMISTRY (2006)
β-Secretase inhibitors:: Modification at the P4 position and improvement of inhibitory activity in cultured cells
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Design and synthesis of potent β-secretase (BACE1) inhibitors with P1′ carboxylic acid bioisosteres
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
A specific amyloid-β protein assembly in the brain impairs memory
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NATURE (2006)
The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice
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JOURNAL OF NEUROCHEMISTRY (2006)
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BIOCHEMISTRY (2005)
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (β-secretase)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2005)
Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2005)
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JOURNAL OF MEDICINAL CHEMISTRY (2004)
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase
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JOURNAL OF MEDICINAL CHEMISTRY (2004)
In vivo inhibition of Aβ production by memapsin 2 (β-secretase) inhibitors
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JOURNAL OF MEDICINAL CHEMISTRY (2001)
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BIOCHEMISTRY (2001)
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BACE1 is the major β-secretase for generation of Aβ peptides by neurons
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