676530-73-7Relevant academic research and scientific papers
Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion Inhibitor: A promising strategy for discovering new antiviral therapeutics
Wang, Chao,Lu, Lu,Na, Heya,Li, Xiangpeng,Wang, Qian,Jiang, Xifeng,Xu, Xiaoyu,Yu, Fei,Zhang, Tianhong,Li, Jinglai,Zhang, Zhenqing,Zheng, Baohua,Liang, Guodong,Cai, Lifeng,Jiang, Shibo,Liu, Keliang
, p. 7342 - 7354 (2015/01/09)
Triterpene saponins are a major group of active components in natural products with nonspecific antiviral activities, while T20 peptide (enfuvirtide), which contains a helix zone-binding domain (HBD), is a gp41-specific HIV-1 fusion inhibitor. In this paper, we report the design, synthesis, and structure-activity relationship (SAR) of a group of hybrid molecules in which bioactive triterpene sapogenins were covalently attached to the HBD-containing peptides via click chemistry. We found that either the triterpenes or peptide part alone showed weak activity against HIV-1 Env-mediated cell-cell fusion, while the hybrids generated a strong cooperative effect. Among them, P26-BApc exhibited anti-HIV-1 activity against both T20-sensitive and -resistant HIV-1 strains and improved pharmacokinetic properties. These results suggest that this scaffold design is a promising strategy for developing new HIV-1 fusion inhibitors and possibly novel antiviral therapeutics against other viruses with class I fusion proteins.
Facile Synthesis of Ginsenoside Ro
Peng, Wenjie,Sun, Jiansong,Lin, Feng,Han, Xiuwen,Yu, Biao
, p. 259 - 262 (2007/10/03)
Two concise synthetic routes, being different in the glycosylation sequence, toward ginsenoside Ro (1) are developed. These syntheses feature the elaboration of the glucuronide residue at a later stage via the TEMPO-mediated selective oxidation and the installation of AZMB as a benzoylic neighboring participating group capable of being selectively removed afterward.
