Ju, Han; Hou, Lingxin; Zhao, Fabao; Zhang, Ying; Jia, Ruifang; Guizzo, Laura; Bonomini, Anna; Zhang, Jiwei; Gao, Zhen; Liang, Ruipeng; Bertagnin, Chiara; Kong, Xiujie; Ma, Xiuli; Kang, Dongwei; Loregian, Arianna; Huang, Bing; Liu, Xinyong; Zhan, Peng published an article in 2022. The article was titled 《Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors via Targeting 150-Cavity》, and you may find the article in Journal of Medicinal Chemistry.Recommanded Product: 197958-29-5 The information in the text is summarized as follows:
With our continuous endeavors in seeking neuraminidase (NA) inhibitors, we reported herein three series of novel oseltamivir amino derivatives with the goal of exploring the druggable chem. space inside the 150-cavity of influenza virus NAs. Among them, around half of the compounds in series C were demonstrated to be better inhibitors against both wild-type and oseltamivir-resistant group-1 NAs than oseltamivir carboxylate (OSC). Notably, compounds 12d, 12e, 15e, and 15i showed more potent or equipotent antiviral activity against H1N1, H5N1, and H5N8 viruses compared to OSC in cellular assays. Furthermore, compounds 12e and 15e exhibited high metabolic stability in human liver microsomes (HLMs) and low inhibitory effect on main cytochrome P 450 (CYP) enzymes, as well as low acute/subacute toxicity and certain antiviral efficacy in vivo. Also, pharmacokinetic (PK) and mol. docking studies were performed. Overall, 12e (I) and 15e (II) possess great potential to serve as anti-influenza candidates and are worthy of further investigation. In the experiment, the researchers used many compounds, for example, 2-Pyridinylboronic acid(cas: 197958-29-5Recommanded Product: 197958-29-5)
2-Pyridinylboronic acid(cas: 197958-29-5) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Recommanded Product: 197958-29-5