2,2-Diphenyl-1-picrylhydrazyl hydrate, a stable free radical, is an alpha-glucosidase inhibitor.

Glycosidases play a pivotal role in processing of various glycoproteins and glycolipids. It is well known that glycosidases are also involved in a variety of degenerative metabolic disorders such as cancer and AIDS. In order to develop potent alpha-glucosidase inhibitors, we first screened 2,2-diphenyl-1-picrylhydrazyl hydrate as a candidate. 2,2-Diphenyl-1-picrylhydrazyl hydrate was found to inhibit alpha- and beta-glucosidases as well as alpha- and beta-mannosidases. It was also shown to be a non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 1.1 x 10(-6) M. Taken together, we anticipate that 2,2-diphenyl-1-picrylhydrazyl hydrate may be a potent inhibitor for some incurable metabolic disorders including AIDS.
AuthorsD S Lee, N S Kim, S H Lee
JournalBiological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 24 Issue 6 Pg. 727-8 (Jun 2001) ISSN: 0918-6158 [Print] Japan
PMID11411571 (Publication Type: Journal Article)
Chemical References
  • Biphenyl Compounds
  • Enzyme Inhibitors
  • Free Radicals
  • Glycoside Hydrolase Inhibitors
  • Picrates
  • 2,2-diphenyl-1-picrylhydrazyl
  • Bepridil
  • Bepridil (analogs & derivatives, chemistry, pharmacology)
  • Biphenyl Compounds
  • Enzyme Inhibitors (pharmacology)
  • Free Radicals
  • Glycoside Hydrolase Inhibitors
  • Kinetics
  • Picrates

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