| abstract |
The invention discloses chiral chloroquine, hydroxychloroquine or pharmaceutically acceptable salts thereof in the preparation of medicines for preventing and/or treating coronavirus pneumonia, using 3CL hydrolase (Mpro), a key drug target of coronavirus, as an action target. application. Both chiral chloroquine and hydroxychloroquine have strong binding strength to Mpro that causes inflammation in the lungs, and can significantly inhibit the activity of Mpro, indicating that they have the effect of preventing and treating pneumonia caused by coronavirus and can be used as an anti-pneumonia drug. By evaluating the inhibitory activity of hERG potassium channel, the concentrations of chloroquine, hydroxychloroquine and their enantiomers that may cause cardiotoxicity to hERG potassium channel are provided. The preparation of chiral chloroquine and hydroxychloroquine by chiral high performance liquid chromatography and chiral synthesis, the S-configuration chloroquine, hydroxychloroquine or its salt can be selected as a single drug, or a pharmaceutical composition can be formed for the treatment of diseases caused by coronavirus , due to its stronger activity and less cardiotoxicity, the range of administration doses is greatly broadened. |