Developing β-secretase inhibitors for treatment of Alzheimer’s disease

Treating transgenic Alzheimer mice with a β-secretase inhibitor, what have we learned?

(2016) Jordan Tang et al.   Aging-US

Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer’s disease

(2010) Wenhai Huang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Investigation of α-phenylnorstatine and α-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors

(2010) Fredrik Wångsell et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization

(2010) Jared Cumming et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

(2010) Anh P. Truong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a sub-micromolar, non-peptide inhibitor of β-secretase with low neural cytotoxicity through in silico screening

(2010) Weijun Xu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors

(2010) Hong Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors

(2010) Stephen Hanessian et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular docking and structure–activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors

(2010) Weijun Xu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

β-Secretase (BACE-1) inhibitory effect of biflavonoids

(2010) Hiroaki Sasaki et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

β-Secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice

(2010) Wan-Pin Chang et al.   FASEB JOURNAL

Design and Synthesis of Potent and Selective BACE-1 Inhibitors

(2010) Catarina Björklund et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Noncompetitive BACE1 Inhibitor TAK-070 Ameliorates A  Pathology and Behavioral Deficits in a Mouse Model of Alzheimer's Disease

(2010) H. Fukumoto et al.   JOURNAL OF NEUROSCIENCE

Predicting memapsin 2 (β-secretase) hydrolytic activity

(2010) Xiaoman Li et al.   PROTEIN SCIENCE

Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and β-secretase

(2009) Yiping Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic

(2009) Fredrik Wångsell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of cell potent BACE-1 inhibitors: Structure–activity relationship of P1′ substituents

(2009) Jennifer M. Sealy et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening

(2009) N. Yi Mok et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application

(2009) Andreas Lerchner et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

P2′-truncated BACE-1 inhibitors with a novel hydroxethylene-like core

(2009) Jenny Adrian Meredith et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core

(2009) Fredrik Wångsell et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Aminoimidazoles as Potent and Selective Human β-Secretase (BACE1) Inhibitors

(2009) Michael S. Malamas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human β-Secretase (BACE1) Inhibitors

(2009) Michael S. Malamas et al.   JOURNAL OF MEDICINAL CHEMISTRY

BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells

(2008) Paul Beswick et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)

(2008) Brian Clarke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors

(2008) J.N. Cumming et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character

(2008) Brian Clarke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

α-Naphthylaminopropan-2-ol Derivatives as BACE1 Inhibitors

(2008) Valentina Asso et al.   ChemMedChem

Evolution of Tertiary Carbinamine BACE-1 Inhibitors: Aβ Reduction in Rhesus CSF upon Oral Dosing

(2008) Philippe G. Nantermet et al.   ChemMedChem

γ-Secretase Inhibition and Modulation for Alzheimers Disease

(2008) Michael Wolfe   Current Alzheimer Research

Second Generation of Hydroxyethylamine BACE-1 Inhibitors: Optimizing Potency and Oral Bioavailability†

(2008) Nicolas Charrier et al.   JOURNAL OF MEDICINAL CHEMISTRY

First Demonstration of Cerebrospinal Fluid and Plasma A  Lowering with Oral Administration of a  -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates

(2008) S. Sankaranarayanan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

β-Secretase as a therapeutic target for Alzheimer’s disease

(2008) Arun K. Ghosh et al.   Neurotherapeutics

Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the substrate binding pocket

(2007) Lee D. Jennings et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor

(2007) U. Iserloh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

(2007) Derek C. Cole et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent memapsin 2 (β-secretase) inhibitors: Design, synthesis, protein-ligand X-ray structure, and in vivo evaluation

(2007) Arun K. Ghosh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent pyrrolidine- and piperidine-based BACE-1 inhibitors

(2007) U. Iserloh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS