Downloads provided by UsageCountsA small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
Copyright policy ) G. P. Chiriano; DE SIMONE, ANGELA; MANCINI, FRANCESCA; D. I. Perez; CAVALLI, ANDREA; BOLOGNESI, MARIA LAURA; G. Legname; +4 Authors
G. P. Chiriano; DE SIMONE, ANGELA; MANCINI, FRANCESCA; D. I. Perez; CAVALLI, ANDREA; BOLOGNESI, MARIA LAURA; G. Legname; A. Martinez; ANDRISANO, VINCENZA; P. Carloni; ROBERTI, MARINELLA;
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as β-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising activities in both enzymatic and cellular assays. Moreover, one of them exhibited the capability to cross the blood-brain barrier as assessed by the parallel artificial membrane permeability assay.
Spain, Italy
Models, Molecular, Neurons, Alzheimer's disease; Amyloid-beta peptide; Drug design; Hit identification; 2-Aminoimidazole, Spectrometry, Mass, Electrospray Ionization, Amyloid beta-Peptides, Magnetic Resonance Spectroscopy, Cell Survival, Imidazoles, Alzheimer's disease;; Amyloid-beta peptide;; Drug design;; Hit identification;; 2-Aminoimidazole, Small Molecule Libraries, Inhibitory Concentration 50, Structure-Activity Relationship, Alzheimer's disease,; Amyloid-beta peptide,; Drug design,; Hit identification,; 2-Aminoimidazole, Alzheimer Disease, Spectroscopy, Fourier Transform Infrared, Animals, Humans, Amyloid Precursor Protein Secretases, Chickens
Models, Molecular, Neurons, Alzheimer's disease; Amyloid-beta peptide; Drug design; Hit identification; 2-Aminoimidazole, Spectrometry, Mass, Electrospray Ionization, Amyloid beta-Peptides, Magnetic Resonance Spectroscopy, Cell Survival, Imidazoles, Alzheimer's disease;; Amyloid-beta peptide;; Drug design;; Hit identification;; 2-Aminoimidazole, Small Molecule Libraries, Inhibitory Concentration 50, Structure-Activity Relationship, Alzheimer's disease,; Amyloid-beta peptide,; Drug design,; Hit identification,; 2-Aminoimidazole, Alzheimer Disease, Spectroscopy, Fourier Transform Infrared, Animals, Humans, Amyloid Precursor Protein Secretases, Chickens
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These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
Influence provided by BIP!impulseImpulse provided by BIP!
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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