title: Synthesis and biological evaluation of 5'-glycyl derivatives of uridine as inhibitors of 1,4-β-galactosyltransferase.
abstract: New 5'-glycyl derivatives of uridine containing fragments of varying lipophilicity were synthesized as analogues of natural peptidyl antibiotics. One of the studied compounds, 5'-O-(N-succinylglycyl)-2',3'-O-isopropylideneuridine (A4), showed moderate inhibition against 1,4-β-galactosyltransferase. However, additional studies showed that the observed inhibitory effect was due to binding to bovine serum albumin, which was used in assays as a stabilizer.
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Jadwiga
authors.initials: J
authors.lastname: Paszkowska
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kral
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Bieg
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Karolina
authors.initials: K
authors.lastname: Żaba
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Węgrzyk
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
authors.forename: Natalia
authors.initials: N
authors.lastname: Jaśkowiak
authors.affiliation: Department of Chemical Sciences, University of Naples Federico II, Via Cintia 4, 80126 Naples, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Molinaro
authors.affiliation: Department of Chemical Sciences, University of Naples Federico II, Via Cintia 4, 80126 Naples, Italy.
authors.forename: Alba
authors.initials: A
authors.lastname: Silipo
authors.affiliation: Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland. Electronic address: ilona.wandzik@polsl.pl.
authors.forename: Ilona
authors.initials: I
authors.lastname: Wandzik
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D014529:Uridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D005700:Galactosyltransferases; D014529:Uridine
keywords: Glycosyltransferase inhibitors; Peptidyl nucleoside; Uridine