The evolution of amidine-based brain penetrant BACE1 inhibitors.
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Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugsDevelopment and Structural Modification of BACE1 InhibitorsHow many molecules does it take to tell a story? Case studies, language, and an epistemic view of medicinal chemistry.IL-17A is implicated in lipopolysaccharide-induced neuroinflammation and cognitive impairment in aged rats via microglial activation.Physiological Functions of the β-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2Swedish mutant APP-based BACE1 binding site peptide reduces APP β-cleavage and cerebral Aβ levels in Alzheimer's mice.Future Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors.A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in RodentsAmyloid beta modulators and neuroprotection in Alzheimer's disease: a critical appraisal.Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics.In silico ligand-based modeling of hBACE-1 inhibitors.Population density analysis for determining the protonation state of the catalytic dyad in BACE1-tertiary carbinamine-based inhibitor complex.Tandem Coupling of Azide with Isonitrile and Boronic Acid: Facile Access to Functionalized Amidines.One-Pot Synthesis of Cyclopropane-Fused Cyclic Amidines: An Oxidative Carbanion Cyclization.Synthesis of amino heterocycle aspartyl protease inhibitors.BACE1 Inhibitor Lanabecestat (AZD3293) in a Phase 1 Study of Healthy Japanese Subjects: Pharmacokinetics and Effects on Plasma and Cerebrospinal Fluid Aβ Peptides.A Versatile Approach to CF3 -Containing 2-Pyrrolidones by Tandem Michael Addition-Cyclization: Exemplification in the Synthesis of Amidine Class BACE1 Inhibitors.AZD3293: Pharmacokinetic and Pharmacodynamic Effects in Healthy Subjects and Patients with Alzheimer's Disease.Palladium-catalyzed three-component reaction of N-tosyl hydrazones, isonitriles and amines leading to amidines.A comparative molecular dynamics study on BACE1 and BACE2 flap flexibility.Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment.Molecular Docking and Dynamic Simulation of AZD3293 and Solanezumab Effects Against BACE1 to Treat Alzheimer's Disease.
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P2860
The evolution of amidine-based brain penetrant BACE1 inhibitors.
description
article científic
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article scientifique
@fr
articol științific
@ro
articolo scientifico
@it
artigo científico
@gl
artigo científico
@pt
artigo científico
@pt-br
artikel ilmiah
@id
artikull shkencor
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artículo científico
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name
The evolution of amidine-based brain penetrant BACE1 inhibitors.
@en
type
label
The evolution of amidine-based brain penetrant BACE1 inhibitors.
@en
prefLabel
The evolution of amidine-based brain penetrant BACE1 inhibitors.
@en
P2093
P1476
The evolution of amidine-based brain penetrant BACE1 inhibitors.
@en
P2093
Daniel Oehlrich
Hana Prokopcova
Harrie J M Gijsen
P304
P356
10.1016/J.BMCL.2014.03.025
P407
P577
2014-03-20T00:00:00Z