A series of C-terminal amino alcohol dipeptide A beta inhibitors.
Potent, small molecule A beta 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.
Garofalo
Albert W
AW
Elan, 800 Gateway Blvd, South San Francisco, CA 94080, USA. al.garofalo@elan.com
Wone
David W G
DW
Phuc
Angela
A
Audia
James E
JE
Bales
Cheryl A
CA
Dovey
Harry F
HF
Dressen
Darren B
DB
Folmer
Beverly
B
Goldbach
Erich G
EG
Guinn
Ashley C
AC
Latimer
Lee H
LH
Mabry
Thomas E
TE
Nissen
Jeffrey S
JS
Pleiss
Michael A
MA
Sohn
Stephen
S
Thorsett
Eugene D
ED
Tung
Jay S
JS
Wu
Jing
J
D000605:Amino Alcohols / Q000138:chemical synthesis* / Q000494:pharmacology*; D053829:Amyloid Precursor Protein Secretases; D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000235:genetics; D016282:Aspartic Acid Endopeptidases; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D010450:Endopeptidases / Q000378:metabolism; D006801:Humans; D009154:Mutation; D013329:Structure-Activity Relationship; D014162:Transfection
D000605:Amino Alcohols; D016229:Amyloid beta-Peptides; D004151:Dipeptides; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human