Université Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Pères, 75006 Paris, France.
Org Biomol Chem. 2011 Dec 21;9(24):8301-12. doi: 10.1039/c1ob06124k. Epub 2011 Nov 1.
Stable analogs of bacterial transferase MraY substrate or product with a pyrophosphate surrogate in their structure are described. β-ketophosphonates were designed as pyrophosphate bioisosteres and were investigated as UDP-GlcNAc mimics. The developed strategy allows introduction of structural diversity at a late stage of the synthesis. The biological activity of the synthesized compounds was evaluated on the MraY enzyme.
本文描述了结构中含有焦磷酸类似物的细菌转移酶 MraY 底物或产物的稳定类似物。β-酮膦酸酯被设计为焦磷酸盐的生物等排体，并被研究作为 UDP-GlcNAc 的模拟物。所开发的策略允许在合成的后期阶段引入结构多样性。合成化合物的生物活性在 MraY 酶上进行了评估。
