Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction (Q27676383)

21

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Leonard Favreau

25

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Lynn A. Hyde

23

object named as

Lynn A Hyde

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author name string

Andrew W Stamford

1

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Jack D Scott

2

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Sarah W Li

3

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Suresh Babu

4

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Dawit Tadesse

5

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Rachael Hunter

6

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Yusheng Wu

7

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Jeffrey Misiaszek

8

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Jared N Cumming

9

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Eric J Gilbert

10

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Chunli Huang

11

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Brian A McKittrick

12

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Liwu Hong

13

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Tao Guo

14

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Zhaoning Zhu

15

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Peter Orth

17

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Johannes H Voigt

18

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Matthew E Kennedy

19

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Xia Chen

20

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Robert Hodgson

22

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Kathleen Cox

24

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Eric M Parker

26

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William J Greenlee

ACS Medicinal Chemistry Letters

27

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publication date

8 November 2012

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published in

1 reference

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor

Crossref

volume

3

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issue

11

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page(s)

897-902

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cites work

1 reference

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Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

20 March 2017

1 reference

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Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors

20 March 2017

1 reference

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Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors

20 March 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3568987

Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation

20 March 2017

1 reference

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Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors

20 March 2017

1 reference

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Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase

20 March 2017

1 reference

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Amyloid-beta protein dimers isolated directly from Alzheimer's brains impair synaptic plasticity and memory

20 March 2017

1 reference

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Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency

20 March 2017

1 reference

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The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics

20 March 2017

1 reference

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Alzheimer's disease: genes, proteins, and therapy

20 March 2017

1 reference

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BACE knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for Alzheimer's disease therapeutics

20 March 2017

1 reference

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Control of peripheral nerve myelination by the beta-secretase BACE1

20 March 2017

1 reference

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A specific amyloid-beta protein assembly in the brain impairs memory

20 March 2017

1 reference

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Diffusible, nonfibrillar ligands derived from Abeta1-42 are potent central nervous system neurotoxins

20 March 2017

1 reference

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The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

7 April 2017

1 reference

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Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011).

7 April 2017

1 reference

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BACE1: the beta-secretase enzyme in Alzheimer's disease

29 September 2017

1 reference

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Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.

29 September 2017

1 reference

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Cassette-accelerated rapid rat screen: a systematic procedure for the dosing and liquid chromatography/atmospheric pressure ionization tandem mass spectrometric analysis of new chemical entities as part of new drug discovery

29 September 2017

1 reference

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BACE1 is the major beta-secretase for generation of Abeta peptides by neurons

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3568987

Mice deficient in BACE1, the Alzheimer's beta-secretase, have normal phenotype and abolished beta-amyloid generation

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3568987

Bace1 modulates myelination in the central and peripheral nervous system.

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3568987

Asymmetric synthesis of beta-amino acid derivatives incorporating a broad range of substitution patterns by enolate additions to tert-butanesulfinyl imines

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3568987

27 November 2018

1 reference

https://pubmed.ncbi.nlm.nih.gov/23412139

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Strategies to optimize the brain availability of central nervous system drug candidates

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23412139