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.

Synthesis and biological evaluation of 5-glycyl derivatives of uridine as inhibitors of 1,4-beta-galactosyltransferase / J., Paszkowska; K., Kral; T., Bieg; K., Zaba; K., Wegrzyk; N., Jakowiak; Molinaro, Antonio; Silipo, Alba; Ilona, Wandzik. - In: BIOORGANIC CHEMISTRY. - ISSN 0045-2068. - 58:(2015), pp. 18-25. [10.1016/j.bioorg.2014.11.001]

Synthesis and biological evaluation of 5-glycyl derivatives of uridine as inhibitors of 1,4-beta-galactosyltransferase

MOLINARO, ANTONIO;SILIPO, ALBA;
2015

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.
2015
Synthesis and biological evaluation of 5-glycyl derivatives of uridine as inhibitors of 1,4-beta-galactosyltransferase / J., Paszkowska; K., Kral; T., Bieg; K., Zaba; K., Wegrzyk; N., Jakowiak; Molinaro, Antonio; Silipo, Alba; Ilona, Wandzik. - In: BIOORGANIC CHEMISTRY. - ISSN 0045-2068. - 58:(2015), pp. 18-25. [10.1016/j.bioorg.2014.11.001]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/596558
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