1440434-28-5

Upstream product

• 1011574-38-1 2-ethyl-N-(2-hydroxy-5-nitrophenyl)butanamide 
• 105-39-5 chloroacetic acid ethyl ester 
• 99-57-0 2-hydroxy-5-nitroaniline 
• 2736-40-5 chlorure d'acide ethyl-2 butyrique 

Downstream Products

• 1440434-32-1 C₂₉H₃₄N₂O₉ 
• 1440434-25-2 (E)-2-(4-(3-(3,4-dihydroxyphenyl)acrylamido)-2-(2-ethylbutanamido)phenoxy)acetic acid 

Relevant academic research and scientific papers

Further discovery of caffeic acid derivatives as novel influenza neuraminidase inhibitors

Eight series of compounds, each series containing two to five compounds were prepared by structural modifications of a lead, which was previously discovered as a mild influenza neuraminidase (NA) inhibitor. On the basis of the biological result, a detailed structure-activity relationship (SAR) was derived and discussed. Several caffeic acid derivatives that acted as non-competitive inhibitors were close or superior to the lead and also presented good antiviral activities in cells. Besides, it was interesting to find that modifications of the lead with different strategies could result in selective inhibition against N1 or N2. The preliminary docking analysis indicated that the 150-cavity of the enzymes played an important role in the selective inhibition.

Caffeic acid derivatives: A new type of influenza neuraminidase inhibitors

Recently, many natural products, especially some plant-derived polyphenols have been found to exert antiviral effects against influenza virus and show inhibitory activities on neuraminidases (NAs). In our research, we took caffeic acid which contained two phenolic hydroxyl groups as the basic fragment to build a small compound library with various structures. The enzyme inhibition result indicated that some compounds exhibited moderate activities against NA and compound 15d was the best with IC50 = 7.2 μM and 8.5 μM against N2 and N1 NAs, respectively. The 3,4-dihydroxyphenyl group from caffeic acid was important for the activity according to the docking analysis. Besides, compound 15d was found to be a non-competitive inhibitor with Ki = 11.5 ± 0.25 μM by the kinetic study and also presented anti-influenza virus activity in chicken embryo fibroblast cells. It seemed promising to discover more potent NA inhibitors from caffeic acid derivatives to cope with influenza virus.