Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2489-93. doi: 10.1016/s0960-894x(01)00477-2.

Abstract

A collection of (2R,3R,4S)-3,4-dihydroxypyrrolidin-2-yl derivatives have been tested for their inhibitory activities toward 25 glycosidases. Competitive (K(i)=7.4 microM) and selective inhibition of alpha-mannosidase from jack bean has been found for (2R,3R,4S)-2-[(benzylamino)methyl]pyrrolidine-3,4-diol and other derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Inhibitory Concentration 50
  • Mannosidases / antagonists & inhibitors*
  • Structure-Activity Relationship
  • alpha-Mannosidase

Substances

  • Enzyme Inhibitors
  • Mannosidases
  • alpha-Mannosidase