Synthesis and preliminary biological evaluations of 5'-substituted derivatives of uridine as glycosyltransferase inhibitors

Molecules. 2013 Jul 8;18(7):8018-27. doi: 10.3390/molecules18078018.

Abstract

New derivatives of uridine which contain a b-ketoenol motif were synthesized, characterized and biologically tested. Synthesized compounds 1-4 showed no activity against bovine milk β-1,4-galactosyltransferase I at concentrations up to 2.0 mM and were not active against Candida albicans and Aspergilus fumigatus up to the maximum tested concentration of 1,000 µg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Aspergillus fumigatus / drug effects
  • Candida albicans / drug effects
  • Cattle
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Glycosyltransferases / antagonists & inhibitors*
  • Glycosyltransferases / metabolism
  • Milk / drug effects
  • Milk / enzymology
  • Structure-Activity Relationship
  • Uridine / analogs & derivatives
  • Uridine / chemical synthesis*
  • Uridine / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Enzyme Inhibitors
  • Glycosyltransferases
  • Uridine