Ontology highlight
ABSTRACT:
SUBMITTER: Goddard-Borger ED
PROVIDER: S-EPMC3380069 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Goddard-Borger Ethan D ED Tropak Michael B MB Yonekawa Sayuri S Tysoe Christina C Mahuran Don J DJ Withers Stephen G SG
Journal of medicinal chemistry 20120306 6
A highly divergent route to lipophilic iminosugars that utilizes the thiol-ene reaction was developed to enable the rapid synthesis of a collection of 16 dideoxyiminoxylitols bearing various different lipophilic substituents. Enzyme kinetic analyses revealed that a number of these products are potent, low-nanomolar inhibitors of human glucocerebrosidase that stabilize the enzyme to thermal denaturation by up to 20 K. Cell based assays conducted on Gaucher disease patient derived fibroblasts demo ...[more]