苯并噻二唑类化合物抗SARS-CoV-2 木瓜样蛋白酶活性研究

SARS-CoV-2 has resulted in millions of deaths and led to rampant economic damage worldwide. The development of small molecule oral drugs has become the main therapeutic strategy for COVID-19. In this paper, based on durg repurposing, we screened our in-house protein tyrosine phosphatase regulator library and indentified several benzothiadiazole derivatives with inhibitory activity against SARS-CoV-2 Papain-like Protease . Among them, the representative compounds 1 and 6 exhibited inhibitory activities against SARS-CoV-2 Papain-like Proteasewith IC50 values of 1.66±0.02μM and 2.07±0.13μM, and blocked 63.05%and70.37%of C-Tan-nCov Wuhan strain 01virusreplicationat a concentration of 10 μM. These preliminary results could provide a possible opportunity for the development of novel SARS-CoV-2 Papain-like Protease inhibitors.