Solid-phase synthesis of aspartic peptidase inhibitors: 3-alkoxy-4-aryl piperidines.
[reaction: see text]. The 3-alkoxy-4-aryl piperidines are non-peptide peptidomimetic inhibitors of several aspartic peptidases. The solid-phase functionalization of 3,4-disubstituted piperidine scaffolds using a traceless linker strategy is described. Synthesis of diverse analogues based on this scaffold provides the potential to generate selective inhibitors of this important class of peptidase.
Bursavich
M G
MG
Department of Chemistry, University of Wisconsin-Madison, 1101 University Avenue, Madison, Wisconsin 53706, USA.
Rich
D H
DH
D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry
D010880:Piperidines; D011480:Protease Inhibitors; D016282:Aspartic Acid Endopeptidases