|کد مقاله||کد نشریه||سال انتشار||مقاله انگلیسی||ترجمه فارسی||نسخه تمام متن|
|1370666||981824||2011||6 صفحه PDF||سفارش دهید||دانلود رایگان|
One of the obvious disadvantages of natural peptides is their liability to proteases. Among the several solutions for this issue, peptoids or oligomers of N-substituted glycine have emerged as a promising tool that may enhance the stability of proteolysis-susceptible natural peptides. We have synthesized the drosocin and its glyco-peptoid analogues linked O-GalNAc at the Thr11 residue. One of our glyco-peptoid analogues showed an increased antibacterial activity by the modification of the Thr11 residue with glyco-peptoid. Structure–activity relationship studies revealed that the antibacterial activity by glyco-peptoid drosocin requires three key elements: free hydroxyl group on the carbohydrate moiety, γ-methyl group of the Thr11 residue derivative and (S)-configuration over (R)-configuration.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 20, 15 October 2011, Pages 6148–6153