Shaanxi Panlong Pharmaceutical Co., Ltd.

Xixian New District Fenghou Original Pharmaceutical Technology Co., Ltd.

Sundian Liu

Chengyuan Liang

Lei Tian

Jingyi Li

Liang Xin

Xiaolin Xie

Dezhu Zhang

Zhao Ma

Kangxiong Wu

Xuhua Zhou

Shaojun Zhang

Xiuding Yang

Yuting Liu

Boyang Li

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 3CLactivity, and is useful in the preparation of a SARS-CoV-2 3CLinhibitor 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 3CLinhibitors and anti-SARS-CoV-2 drugs.

3-tetrazolylmethyl-1,3,5-triazin-2,4-dione compound inhibiting coronavirus 3CL protease activity and preparation method and use thereof

Disclosed is a compound of formula I, a pharmaceutically acceptable salt, or a tautomer thereof. formula I. R, R, Rand Rare independently selected from the group consisting of hydrogen, methyl group, tert-butyl group, methoxy group, difluoromethyl, trifluoromethyl, trifluoromethoxy, nitro, halogen, phenyl and aromatic heterocyclic; Ris a hydrogen or halogen; and Ris hydrogen, C1-4 alkane or C1-4 cycloalkane.

3-triazolyl methyl-1,3,5-triazine-2,4-dione compounds and preparation method and application thereof

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Xi'an, China

Sundian Liu