2573-30-0Relevant academic research and scientific papers
Discovery and evolution of 12N-substituted aloperine derivatives as anti-SARS-CoV-2 agents through targeting late entry stage
Wang, Kun,Wu, Jia-Jing,Xin–Zhang,Zeng, Qing-Xuan,Zhang, Na,Huang, Wei-Jin,Tang, Sheng,Wang, Yan-Xiang,Kong, Wei-Jia,Wang, You-Chun,Li, Ying-Hong,Song, Dan-Qing
, (2021/08/03)
So far, there is still no specific drug against COVID-19. Taking compound 1 with anti-EBOV activity as the lead, fifty-four 12N-substituted aloperine derivatives were synthesized and evaluated for the anti-SARS-CoV-2 activities using pseudotyped virus model. Among them, 8a exhibited the most potential effects against both pseudotyped and authentic SARS-CoV-2, as well as SARS-CoV and MERS-CoV, indicating a broad-spectrum anti-coronavirus profile. The mechanism study disclosed that 8a might block a late stage of viral entry, mainly via inhibiting host cathepsin B activity rather than directly targeting cathepsin B protein. Also, 8a could significantly reduce the release of multiple inflammatory cytokines in a time- and dose-dependent manner, such as IL-6, IL-1β, IL-8 and MCP-1, the major contributors to cytokine storm. Therefore, 8a is a promising agent with the advantages of broad-spectrum anti-coronavirus and anti-cytokine effects, thus worthy of further investigation.
Preparation method of N-aryl glycine ester derivative
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Paragraph 0041-0046, (2020/07/12)
The invention relates to a preparation method of an N-aryl glycine ester derivative. The invention aims to solve the problems of complex steps and environmental pollution in the existing method for synthesizing the N-aryl glycine ester derivative. The preparation method comprises the following steps: dissolving an aryl primary amine compound, ethyl diazoacetate, a reaction aid and a photocatalystin an organic solvent at room temperature, uniformly mixing, reacting under a blue LEDs lamp, carrying out reduced pressure distillation to remove the solvent, and separating and purifying to obtain the product. The problems of high energy consumption, high cost and environmental pollution caused by high temperature, biocatalyst or metal organic framework required by the synthesis of the existingN-aryl glycine ester derivative are solved. A route for synthesizing the N-arylglycine ester derivative, which is green, efficient, mild in condition, simple in method, convenient to operate and highin yield, is found, and the method is applied to the field of organic synthesis.
