尿苷 5'-糖基衍生物的合成及作为 1,4-β-半乳糖基转移酶抑制剂的生物评价。
Synthesis and biological evaluation of 5'-glycyl derivatives of uridine as inhibitors of 1,4-β-galactosyltransferase.
机构信息
Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
Department of Chemical Sciences, University of Naples Federico II, Via Cintia 4, 80126 Naples, Italy.
出版信息
Bioorg Chem. 2015 Feb;58:18-25. doi: 10.1016/j.bioorg.2014.11.001. Epub 2014 Nov 10.
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.
新型 5'-甘氨酰尿嘧啶类似物，含有不同疏水性片段，被合成作为天然肽类抗生素的类似物。研究的化合物之一，5'-O-(N-琥珀酰甘氨酰)-2',3'-O-亚异丙基尿苷（A4），对 1,4-β-半乳糖基转移酶表现出中等抑制作用。然而，进一步的研究表明，观察到的抑制作用是由于与牛血清白蛋白结合所致，牛血清白蛋白在测定中被用作稳定剂。
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