Chinese Academy of Sciences

Shanghai Lead Discovery Pharmaceuticals Limited Company

Huyabio International, LLC

Huya Bioscience International, LLC

Donglu Bai

Jing Lan Chen

Hong Tao Liu

Hualiang Jiang

Fei Ye

Kaixian Chen

Jingkang Shen

Tao Sun

Jianping Zuo

Jianhua Shen

Yiping Wang

Xu Shen

Xiaomin Luo

Bing Xiong

Lili Chen

Yiming Yang

Haibin Luo

Chunshan Gui

Yifu Yang

Xianhan Zhuang

Xuchang He

Yueli Dong

Weizhou Chen

Yunxin Bu

Aili Kang

The present invention discloses 3D-structure of SARS-CoV Viral 3CL Protease obtained through molecular simulation. The 3D-structure is used as a drug target for screening the existing medical database CMC (Comprehensive Medicinal Chemistry, MDL Information System, Inc.), and a group of compounds which have the activity of inhibiting SARS-CoV virus 3CL Protease are found. Cinanserin was tested at molecular and viral levels, and it was found to be able to inhibit the SARS-CoV viral 3CL protease and SARS-CoV viruses. Cinanserin analogs were synthesized and tested at molecular and viral levels, they were found to be able to inhibit the SARS-CoV virus 3CL Protease and SARS-CoV viruses, and may be used for treating and/or preventing SARS-CoV virus infection.

3D-structure model of SARS coronavirus 3CL protease and anti-SARS drugs

N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.

N-substituted benzyl or phenyl aromatic sulfamides compounds and the use thereof

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Donglu Bai