Synthesis and Biological Evaluation of Umifenovir Analogues as Anti-SARS-CoV-2 Agents.
Hiroaki TanakaSeiya MiyagiYusuke YoshidaJustin Steven LambChristian Nanga ChickLokadi Pierre LuhataMizuho ShibataEri TanakaYumiko SuzukiToyonobu UsukiPublished in: ChemistrySelect (2022)
The unprecedented novel coronavirus disease 2019 (COVID-19) pandemic is a threat to global health and the economy. Since the outbreak of COVID-19, great effort has been made to reposition existing drugs to shorten development timelines, in addition to vaccine development and drug discovery campaigns. Umifenovir is a broad-spectrum antiviral agent used to treat influenza in China and Russia and is currently undergoing clinical trials for the treatment of COVID-19. In this article, the synthesis of umifenovir analogues and their biological evaluation are reported. The inhibitory activities of analogues against the binding of the spike glycoprotein (S-protein) of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) to the ACE2 receptor, which is a possible mode of action for umifenovir to inhibit viral infection, were investigated.
Keyphrases
- respiratory syndrome coronavirus
- sars cov
- coronavirus disease
- global health
- drug discovery
- molecular docking
- clinical trial
- public health
- structure activity relationship
- binding protein
- randomized controlled trial
- angiotensin ii
- protein protein
- study protocol
- angiotensin converting enzyme
- atomic force microscopy
- amino acid