title: Synthesis and preliminary biological evaluations of 5'-substituted derivatives of uridine as glycosyltransferase inhibitors.
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.
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland. jadwiga.paszkowska@polsl.pl
authors.forename: Jadwiga
authors.initials: J
authors.lastname: Paszkowska
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kral
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Bieg
authors.forename: Urszula
authors.initials: U
authors.lastname: Nawrot
authors.forename: Wiesław
authors.initials: W
authors.lastname: Szeja
authors.forename: Ilona
authors.initials: I
authors.lastname: Wandzik
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D002417:Cattle; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D016695:Glycosyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008892:Milk / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship; D014529:Uridine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D016695:Glycosyltransferases; D014529:Uridine