1425864-56-7Relevant academic research and scientific papers
Synthesis of 7-arylimidazo[1,2-a]pyrazin-8(7H)-one derivatives
Kovalenko, Svitlana S.,Drushlyak, Oleksandr G.,Kovalenko, Sergiy M.,Bunyatyan, Natalya D.,Kravchenko, Dmitry V.,Ivachtchenko, Alexandre V.
, p. 386 - 391 (2019)
[Figure not available: see fulltext.] A suitable approach to the synthesis of 7-arylimidazo[1,2-a]pyrazin-8(7H)-ones starting from esters of oxalic acid monoamides via cyclization of intermediate 3-aminopyrazin-2-ones with α-halocarbonyl compounds has bee
Discovery of 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one derivatives as new potent PB2 inhibitors
Yang, Jianhong,Du, Jiatian,Huang, Chong,Wang, Tianqi,Huang, Luyi,Yang, Shengyong,Li, Linli
, p. 1609 - 1613 (2019)
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 12b 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, respectively. In antiviral activity and cellular cytotoxicity assays, compound 12b showed an EC50 value of 1.025 μM and a CC50 value greater than 100 μM. Molecular docking was also used to predict the binding mode of 12b with PB2. Collectively, this study provides a promising lead compound for subsequent anti-influenza drug discovery targeting PB2.
Anti-influenza small molecule compound and preparation method and application thereof
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Paragraph 0225; 0227-0232; 0251-0252, (2020/08/27)
The present invention provides a compound represented by a formula I, or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a prodrug, or a metabolite thereof. The invention also providesa preparation method and application of the compound. The compound prepared by the preparation method has relatively strong binding capacity with PB2 protein, particularly PB2318-483 protein, so thatthe transcription process of influenza RNA polymerase can be blocked, and the proliferation of influenza viruses is further inhibited. The compound can be used for preparing anti-influenza virus medicines.
Synthesis of 4H-pyrazino[1,2-a]pyrimidine-4,9(8H)-diones and imidazo[1,2-a]pyrazin-8(7H)-ones
Raubo, Piotr,Ladwa, Neal
, p. 2935 - 2938 (2013/02/22)
A facile method of synthesis of 4H-pyrazino[1,2-a]-pyrimidine-4,9(8H)- diones and imidazo[1,2-a]pyrazin-8(7H)-ones from the corresponding 3-amino-2(1H)-pyrazinones is described. Georg Thieme Verlag KG · Stuttgart · New York.
