On July 1, 2019, Yang, Jianhong; Du, Jiatian; Huang, Chong; Wang, Tianqi; Huang, Luyi; Yang, Shengyong; Li, Linli published an article.COA of Formula: C5H4Br2N2O The title of the article was Discovery of 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one derivatives as new potent PB2 inhibitors. And the article contained the following:
PB2 is an important subunit of influenza RNA-dependent RNA polymerase (RdRP) and has been recognized as a promising target for the treatment of influenza. We herein report the discovery of a new series of PB2 inhibitors containing the skeleton 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one. Compound I is the most potent one, which showed KD values of 0.11 μM and 0.19 μM in surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) assays, resp. In antiviral activity and cellular cytotoxicity assays, compound I showed an EC50 value of 1.025 μM and a CC50 value greater than 100 μM. Mol. docking was also used to predict the binding mode of I with PB2. Collectively, this study provides a promising lead compound for subsequent anti-influenza drug discovery targeting PB2. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).COA of Formula: C5H4Br2N2O
The Article related to fluoropyrrolopyridinyl pyrazinone preparation pb2 inhibitor antiinfluenza antiviral activity, influenza a virus, pb2, small molecule inhibitor, structure-activity relationship and other aspects.COA of Formula: C5H4Br2N2O