当前位置: X-MOL 学术Org. Biomol. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Nicotinamide riboside–amino acid conjugates that are stable to purine nucleoside phosphorylase
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-04-01 , DOI: 10.1039/d0ob00134a
Faisal Hayat 1 , Marie E Migaud 1
Affiliation  

The nutraceutical Nicotinamide Riboside (NR), an efficacious biosynthetic precursor to NAD, is readily metabolized by the purine nucleoside phosphorylase (PNP). Access to the PNP-stable versions of NR is difficult because the glycosidic bond of NR is easily cleaved. Unlike NR, NRH, the reduced form of NR, offers sufficient chemical stability to allow the successful functionalisation of the ribosyl-moiety. Here, we report on a series of NRH and NR derived amino acid conjugates, generated in good to excellent yields and show that O5′-esterification prevents the PNP-catalyzed phosphorolysis of these NR prodrugs.

中文翻译:

对嘌呤核苷磷酸化酶稳定的烟酰胺核苷-氨基酸缀合物

营养保健品烟酰胺核苷 (NR) 是 NAD 的有效生物合成前体,很容易被嘌呤核苷磷酸化酶 (PNP) 代谢。获得 PNP 稳定版本的 NR 很困难,因为 NR 的糖苷键很容易断裂。与 NR 不同,NRH(NR 的还原形式)提供足够的化学稳定性,以实现核糖基部分的成功官能化。在这里,我们报告了一系列 NRH 和 NR 衍生的氨基酸缀合物,这些缀合物的产率良好至优异,并表明O 5'-酯化可防止这些 NR 前药的 PNP 催化磷酸解。
更新日期:2020-04-24
down
wechat
bug