Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Gerritz, Samuel W
Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis. [electronic resource] - Journal of medicinal chemistry Nov 2012 - 9208-23 p. digital
Publication Type: Journal Article
1520-4804
10.1021/jm300931y doi
Amyloid Precursor Protein Secretases--antagonists & inhibitors
Amyloid beta-Peptides--metabolism
Amyloid beta-Protein Precursor--genetics
Animals
Aspartic Acid Endopeptidases--antagonists & inhibitors
Brain--metabolism
Cell Line
Crystallography, X-Ray
Guanidines--chemical synthesis
Humans
Isoxazoles--chemical synthesis
Models, Molecular
Molecular Structure
Mutation
Peptide Fragments--metabolism
Protein Binding
Radioligand Assay
Rats
Small Molecule Libraries
Solid-Phase Synthesis Techniques
Solutions
Structure-Activity Relationship
Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis. [electronic resource] - Journal of medicinal chemistry Nov 2012 - 9208-23 p. digital
Publication Type: Journal Article
1520-4804
10.1021/jm300931y doi
Amyloid Precursor Protein Secretases--antagonists & inhibitors
Amyloid beta-Peptides--metabolism
Amyloid beta-Protein Precursor--genetics
Animals
Aspartic Acid Endopeptidases--antagonists & inhibitors
Brain--metabolism
Cell Line
Crystallography, X-Ray
Guanidines--chemical synthesis
Humans
Isoxazoles--chemical synthesis
Models, Molecular
Molecular Structure
Mutation
Peptide Fragments--metabolism
Protein Binding
Radioligand Assay
Rats
Small Molecule Libraries
Solid-Phase Synthesis Techniques
Solutions
Structure-Activity Relationship