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Novel pyrimidine derivatives containing an amide moiety: design, synthesis, and antifungal activity

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The objectives of the current study were to synthesize a series of novel pyrimidine derivatives containing an amide moiety and to investigate their in vitro antifungal activities against eight kinds of plant pathogenic fungi via the poison plate technique. The preliminary biological test showed that compounds 4a4aa exhibited moderate-to-good antifungal activities against the tested plant pathogenic fungi compared with the commercial agents. Particularly, compounds 4n, 4q, and 4w exhibited excellent antifungal activity against Phomopsis sp., with the half-maximal effective concentration (EC50) values of 1.8, 1.4, and 1.7 μg/mL, which were even better than that of pyrimethanil (32.1 μg/mL). To the best of our knowledge, this is the first report on the antifungal activity of this series of novel N-acyl 4-(4-aminophenoxy)-2-methyl-6-trifluoromethylpyrimidine derivatives containing an amide moiety.

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We gratefully acknowledge the financial support of the Guizhou Science and Technology Fund Project (No. [2016]1006), the Natural Science Foundation of the Department of Education of Guizhou Province (No. qian jiao he KY word [2016]091), China Postdoctoral Science Foundation (No. 2017M623070), the National Natural Science Foundation of China (Nos. 31701821, 21762037, 21462010), and the Program of Excellent Innovation Talents of Guizhou Province (No. 20164022).

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Correspondence to Guiping Ouyang.

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Wu, W., Chen, M., Wang, R. et al. Novel pyrimidine derivatives containing an amide moiety: design, synthesis, and antifungal activity. Chem. Pap. 73, 719–729 (2019).

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