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Microwave-assisted Synthesis and Antifungal Activity of Novel 1,2,4- Triazole Thioether Derivatives Containing Pyrimidine Moiety

[ Vol. 15 , Issue. 4 ]

Author(s):

Meng Xu, Ya-Bo Zhu, Mei Wang, Ikhlas A. Khan, Xing-Hai Liu and Jian-Quan Weng*   Pages 347 - 352 ( 6 )

Abstract:


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.

Keywords:

Pyrimidine moiety, 1, 2, 4-triazole, thioether, microwave-assisted, synthesis, antifungal activity.

Affiliation:

College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014, College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014, National Center for Natural Products Research, School of Pharmacy, University of Mississippi, Oxford, MS 38677, Division of Pharmacognosy, Department of BioMolecular Sciences, School of Pharmacy, University of Mississippi, Oxford, MS 38677, College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014, College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014

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