Abstract
In this study, 17 novel pyrimidine derivatives containing an amide moiety were synthesized. Then their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinereal (B. cinereal) were determined. A preliminary biological test showed that compounds 5-bromo-2-fluoro-N-(2-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (5f) and 5-bromo-2-fluoro-N-(3-((2-methyl-6-(trifluoromethyl)pyrimidin-4-yl)oxy)phenyl)benzamide (5o) exhibited higher antifungal activity against Phomopsis sp., with an inhibition rate of 100% compared to that of Pyrimethanil at 85.1%. In particular, compound 5o exhibited excellent antifungal activity against Phompsis sp., with the EC50 value of 10.5 μg/ml, which was even better than that of Pyrimethanil (32.1 μg/ml). As far as we know, this is the first report on the antifungal activities against B. dothidea, Phomopsis sp., and B. cinereal of this series of pyrimidine derivatives containing an amide moiety.
Highlights
Plant fungal diseases pose serious threats to crop production and caused huge economic losses throughout the world (Strange and Scott, 2005)
We reported a series of novel pyrimidine derivatives containing an amine moiety (Figure 1) and found that the target compounds revealed certain antifungal, insecticidal, and antiviral activities (Wu et al, 2016a: Wu et al, 2020)
Bioassay results showed that compounds 5i, 5l, 5n, and 5o had good inhibition rates on B. dothidea, with the inhibition rates of 82.1, 81.1, 84.1, and 88.5%, respectively, which were similar to Pyrimethanil (84.4%)
Summary
Plant fungal diseases pose serious threats to crop production and caused huge economic losses throughout the world (Strange and Scott, 2005). Crop cultivators continually battle with plant fungal diseases affecting crops. The available traditional fungicides used for plant fungal diseases control represent a danger to the living system by killing the target fungi and affecting beneficial living systems (Patel et al, 2014). To protect crops from fungal diseases, commercial agriculture relies heavily on the inputs of chemical pesticides. The resistance of plant fungal diseases against fungicides is rapidly becoming a serious problem. The development of novel and promising fungicides is urgently required
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