Parallel synthesis of DAPT derivatives and their γ-secretase- inhibitory activity
Parallel synthesis of the C-terminal-modified DAPT (1) derivatives was accomplished utilizing our novel resin 7. Condensation reaction of the N-acylamino acid 10 with the amines 11a-o proceeded smoothly to give the corresponding amides 6a-o without any epimerization. Among the analogues, the benzophenonemethyl amide derivative 6o showed 30 times more potent activity than the original DAPT (1).
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 assa
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
p. 3051 - 3053
(2007/10/03)
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