A series of C-Terminal amino alcohol dipeptide Aβ inhibitors

Potent, small molecule Aβ inhibitors have been prepared that incorporate an alanine core bracketed by an N-terminal arylacetyl group and various C-terminal amino alcohols. The compounds exhibit stereospecific inhibition as demonstrated in an in vitro assay. Graphic

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-11, Vol.12 (21), p.3051-3053
Main Authors: Garofalo, Albert W., Wone, David W.G., Phuc, Angela, Audia, James E., Bales, Cheryl A., Dovey, Harry F., Dressen, Darren B., Folmer, Beverly, Goldbach, Erich G., Guinn, Ashley C., Latimer, Lee H., Mabry, Thomas E., Nissen, Jeffrey S., Pleiss, Michael A., Sohn, Stephen, Thorsett, Eugene D., Tung, Jay S., Wu, Jing
Format: Article
Language:English
Subjects:
Amino Alcohols - chemical synthesis
Amino Alcohols - pharmacology
Amyloid beta-Peptides - antagonists & inhibitors
Amyloid beta-Peptides - genetics
Amyloid Precursor Protein Secretases
Aspartic Acid Endopeptidases
Cell Line
Cell Survival - drug effects
Dipeptides - chemical synthesis
Dipeptides - pharmacology
Endopeptidases - metabolism
Humans
Mutation
Structure-Activity Relationship
Transfection
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Description
Summary:Potent, small molecule Aβ inhibitors have been prepared that incorporate an alanine core bracketed by an N-terminal arylacetyl group and various C-terminal amino alcohols. The compounds exhibit stereospecific inhibition as demonstrated in an in vitro assay. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00684-4