Abstract: The present invention relates to application of gossypol and its optical isomers to preparation of an anti-Coronavirus drug. Specifically disclosed is application of pharmaceutically acceptable salts, solvates, isotopes, stereoisomers, stereoisomer mixtures, and tautomers of the gossypol and its optical isomers to preparation of a drug for preventing and/or treating a disease caused by a Coronavirus. The Coronavirus is MERS-CoV, SARS-CoV, or SARS-CoV-2. It is found in the present invention for the first time that the gossypol and its optical isomers can inhibit the activity of Coronavirus 3CL proteases to achieve an anti-Coronavirus effect. The half maximal inhibitory concentrations of gossypol and (?)-gossypol to SARS-CoV proteases and SARS-CoV-2 3CL proteases are all lower than 10 ?M. The anti-Coronavirus 3CL protease effect is good. Therefore, the gossypol and its optical isomers have the potential for use in the preparation of a drug for preventing and/or treating novel Coronavirus infections.

Abstract: The present invention relates to the technical field of medicinal chemistry, and particularly to a method for preparing a 3-tetrazolylmethyl-1,3,5-triazin-2,4-dione compound inhibiting coronavirus 3CL protease activity and use thereof. Specifically, a compound of Formula I, or a pharmaceutically acceptable salt, or an optical isomer, or an isotope-substituted form thereof is provided. The compound effectively inhibits the SARS-CoV-2 3CLpro activity, and is useful in the preparation of a SARS-CoV-2 3CLpro inhibitor to block the replication and transcription of SARS-CoV-2 viruses in patients. The compound prepared in the present invention has high in-vitro safety, and very good prospect of application in the preparation of SARS-CoV-2 3CLpro inhibitors and anti-SARS-CoV-2 drugs.

Abstract: Disclosed is a compound of formula I, a pharmaceutically acceptable salt, or a tautomer thereof. formula I. R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen, methyl group, tert-butyl group, methoxy group, difluoromethyl, trifluoromethyl, trifluoromethoxy, nitro, halogen, phenyl and aromatic heterocyclic; R5 is a hydrogen or halogen; and R6 is hydrogen, C1-4 alkane or C1-4 cycloalkane.