Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells

A series of oxadiazole derivatives containing 1,4-benzodioxan (4a-4s) have been designed, synthesized, structurally determined, and their biological activities were also evaluated as potential immunosuppressive agents. All the synthesized compounds were first synthesized. Among the compounds, compound 4i showed the most potent biological activity against RAW264.7 cells (inhibition = 37.66 ± 2.34% for NO overproduction and IC50 = 0.05 μM for iNOS). Docking simulation was performed to position compound 4i into the iNOS structure active site to determine the probable binding model. RT-PCR experiment results demonstrated that some of these compounds possessed good immunosuppressive activity against iNOS, especially for compound 4i. Therefore, compound 4i with potent inhibitory activity may be a potential agent.