Chemistry Section, Laboratory of Comparative Carcinogenesis, National Cancer Institute at Frederick, Frederick, Maryland 21702, USA.
Org Lett. 2010 Jan 1;12(1):56-9. doi: 10.1021/ol902481s.
GlcNAc-PROLI/NO prodrugs that are activated by N-acetylglucosaminidase to release nitric oxide (NO) are described. A classical acid-amine coupling is used to bifunctionalize these PROLI/NO prodrugs, which on activation generate up to 4 mol of NO, a peptide residue, and an N-acetylglucosamine residue. Many of the prodrugs synthesized are efficient sources of intracellular NO.
描述了通过 N-乙酰氨基葡萄糖苷酶激活释放一氧化氮 (NO) 的 GlcNAc-PROLI/NO 前药。使用经典的酸-胺偶联来双功能化这些 PROLI/NO 前药，它们在激活时生成多达 4 摩尔的 NO、一个肽残基和一个 N-乙酰氨基葡萄糖残基。合成的许多前药都是有效的细胞内 NO 来源。
