Shaanxi Panlong Pharmaceutical Co., Ltd.

Shaanxi University of Science and Technology

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

Yuting Liu

Xiuding Yang

Chengyuan Liang

Lei Tian

Jingyi Li

Liang Xin

Xiaolin Xie

Dezhu Zhang

Zhao Ma

Kangxiong Wu

Xuhua Zhou

Shaojun Zhang

Sundian Liu

Yanzi Wang

Kairui Kang

Jiaxuan Li

Ying Zhou

Boyang Li

Chenguan Liang

Changhua Ke

The present invention discloses a pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and a preparation method and use thereof and belongs to the field of medicinal chemistry. A pleuromutilin derivative with thiazole-pyridine benzyl quaternary ammonium salt side chain is successfully prepared by structural reconstruction of pleuromutilin and then structural modification with a quaternary ammonium salt compound. This compound synthesis method has the advantages of easily available raw materials, simple operation and high product yield, and is suitable for industrial production. The results of in vitro pharmacological experiments show that the pleuromutilin derivative of the present invention have good antibacterial and anti-mycoplasma activities, as well as good solubility, and these results show that the pleuromutilin derivative is of great value in the development of an anti-pathogenic microorganism drug.

Pleuromutilin derivative containing thiazole-pyridine benzyl quaternary ammonium salt side chain and preparation method and use thereof

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

Yuting Liu