97-60-9Relevant articles and documents
Functionalized C-nucleosides as remarkable RNA binders: Targeting of prokaryotic ribosomal A-site RNA
Joly, Jean-Patrick,Gaysinski, Marc,Zara, Lorena,Duca, Maria,Benhida, Rachid
supporting information, p. 10432 - 10435 (2019/09/07)
RNA represents an extremely promising and yet challenging therapeutic target. Here, we report the design of a series of C-nucleosides as original RNA binders. Some of them bind strongly and selectively to A-site prokaryotic ribosomal RNA.
Eco-friendly, catalyst and solvent-free, synthesis of acetanilides and N-benzothiazole-2-yl-acetamides
Cunha, Silvio,De Santana, Louren?o L. B.
, p. 1137 - 1144 (2017/05/01)
An expeditious and green synthesis of acetamides in a solvent-free simple way is described, without catalyst or additives, and in good yield by an instantaneous reaction of anilines or 2-aminothiazoles and acetic anhydride without external heating, and with simple purification. Sixteen substituted acetanilides and four N-benzothiazole-2-yl-acetamides were formed, but aliphatic amines of low molecular weight were not as effective as aromatic ones, and only cyclohexylamine and the enaminone ethyl 3-amino-2-butenoate afforded the corresponding acetamides in good yield.
Caffeic acid derivatives: A new type of influenza neuraminidase inhibitors
Xie, Yuanchao,Huang, Bing,Yu, Kexiang,Shi, Fangyuan,Liu, Tianqi,Xu, Wenfang
supporting information, p. 3556 - 3560 (2013/07/04)
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.