Background: Plant diseases caused by plant pathogens are important constraints to agricultural
production throughout the world and at least 10% of global food production is lost to plant
diseases. In order to discover new fungicides and control the plant diseases, a series of novel 1,2,4-
triazole thioether derivatives carrying a pyrimidine moiety were designed and synthesized.
Methods: Thirteen novel 1,2,4-triazole thioether derivatives carrying a pyrimidine moiety were
designed by splicing the active substructure and synthesized under microwave irradiation condition.
Their structures were characterized by 1H-NMR, 13C-NMR, ESI-MS and elemental analysis, and
their antifungal activities were evaluated using the mycelium growth rate test.
Results: These compounds were screened for antifungal activity against Colletotrichum orbiculare,
Botrytis cinerea and Rhizoctonia solani at 50 µg/mL. Some compounds showed moderate to good
antifungal activities. Especially the inhibition rate of compound 7c against C. orbiculare and R. solani
were 80% and 76% respectively.
Conclusion: A practical synthetic route to 1,2,4-triazole thioether derivatives by using the microwave-
assisted method is presented. This study suggests that the 1,2,4-triazole thioether derivatives
exhibited moderate to good inhibition activity against C. orbiculare and R. solani at 50 µg/mL, and could
be further developed as potential fungicides.