Amplification of the inhibitory activity of miglitol by monofluorination.
Selective monofluorination of the alpha-glycosidase inhibitor and antidiabetic agent Miglitol at position C2 creates an competitive inhibitor of five times higher activity than the parent compound. Its screening against a panel of human cell lines showed a low cytotoxicity therefore making this compound an interesting candidate for further clinical investigations.
Prell
Erik
E
Martin-Luther-Universität Halle-Wittenberg, NF II, Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
Csuk
René
R
D017485:1-Deoxynojirimycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D002460:Cell Line; D065089:Glycoside Hydrolase Inhibitors; D054879:Halogenation; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D000520:alpha-Glucosidases / Q000378:metabolism
D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; C045621:miglitol; D017485:1-Deoxynojirimycin; D000520:alpha-Glucosidases