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1.
Bioorg Med Chem Lett ; 20(20): 6034-9, 2010 Oct 15.
Article in English | MEDLINE | ID: mdl-20822903
2.
Bioorg Med Chem Lett ; 19(22): 6386-91, 2009 Nov 15.
Article in English | MEDLINE | ID: mdl-19811916

ABSTRACT

Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Abeta cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1' residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.


Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1/chemistry , Amyloid Precursor Protein Secretases/antagonists & inhibitors , Aspartic Acid Endopeptidases/antagonists & inhibitors , Drug Design , ATP Binding Cassette Transporter, Subfamily B, Member 1/genetics , Amyloid Precursor Protein Secretases/chemistry , Amyloid Precursor Protein Secretases/genetics , Aspartic Acid Endopeptidases/chemistry , Aspartic Acid Endopeptidases/genetics , Humans , Models, Molecular , Molecular Structure , Structure-Activity Relationship , Substrate Specificity
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