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

Abstract

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.

• Authors: D S Lee, N S Kim, S H Lee
• Journal: Biological & pharmaceutical bulletin (Biol Pharm Bull) Vol. 24 Issue 6 Pg. 727-8 (Jun 2001) ISSN: 0918-6158 [Print] Japan
• PMID: 11411571 (Publication Type: Journal Article)

Chemical References

• Biphenyl Compounds
• Enzyme Inhibitors
• Free Radicals
• Glycoside Hydrolase Inhibitors
• Picrates
• Bepridil
• 1,1-diphenyl-2-picrylhydrazyl

Topics

• Bepridil (analogs & derivatives, chemistry, pharmacology)
• Biphenyl Compounds
• Enzyme Inhibitors (pharmacology)
• Free Radicals
• Glycoside Hydrolase Inhibitors
• Kinetics
• Picrates