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.
Lee
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Biophysical Chemistry Laboratory, The Institute of Physical and Chemical Research RIKEN Harima Institute, Sayo, Hyogo, Japan.
Kim
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Lee
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D015764:Bepridil / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D001713:Biphenyl Compounds; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005609:Free Radicals; D065089:Glycoside Hydrolase Inhibitors; D007700:Kinetics; D010851:Picrates
D001713:Biphenyl Compounds; D004791:Enzyme Inhibitors; D005609:Free Radicals; D065089:Glycoside Hydrolase Inhibitors; D010851:Picrates; D015764:Bepridil; C004931:1,1-diphenyl-2-picrylhydrazyl