Synthesis And Biological Activities Of 4-Alkyl-6-Aryl-1,3-Thiazines

A series of 1,3-thiazine derivatives 1a similar to 1p were designed and synthesized by the reaction of aromatic aldehyde via condensation and cyclization, and their inhibitory activity of nueraminidase (NA) and serotonin reuptake (SERT) were evaluated in vitro. The pharmacological results showed that compound 1i exhibits good activity of NA with the inhibitory rate of 68.91% at the concentration of 40 mu g/mL, which is similar to oseltamivir (inhibitory rate is 72.6%), moreover, at the concentration of 10.0 mu g/mL, compounds id, le and if exhibit good serotonin reuptake inhibitory activity with inhibitory rates of 99.5%, 99.6% and 99.8%, respectively.