Abstract
Seventeen novel N-phenylbenzamide derivatives bearing a trifluoromethylpyrimidine moiety were synthesized via four-step reactions. Their antifungal and insecticidal properties were evaluated. Antifungal test results demonstrated that some of the synthesized compounds showed better in vitro bioactivities against Phomopsis sp., Botryosphaeria dothidea (B. dothidea), and Botrytis cinerea (B. cinerea) at 50 μg/mL than pyrimethanil. Unfortunately, the synthesized compounds revealed lower insecticidal activities against Spodoptera frugiperda (S. frugiperda) and Mythimna separata (M. separata) at 500 μg/mL than chlorantraniliprole.
Highlights
Plant fungal diseases and insect pests have drawn widespread attention because of their enormous damage toward agriculture [14]. e traditional commercial fungicides and insecticides used to prevent and control plant diseases could increase the yield, improve the quality of agricultural products, and not reduced huge loss annually [5, 6]
The misuse of traditional fungicides and insecticides had speeded up the resistance of plant diseases, which is rapidly becoming a huge challenge in agriculture [7, 8]
The target compounds 4a–4q were obtained from 2-substituted-4-((6(trifluoromethyl)pyrimidin-4-yl)oxy)benzoic acid (3) and aromatic amines by amidation reaction
Summary
Plant fungal diseases and insect pests have drawn widespread attention because of their enormous damage toward agriculture [14]. e traditional commercial fungicides and insecticides used to prevent and control plant diseases could increase the yield, improve the quality of agricultural products, and not reduced huge loss annually [5, 6]. Many of pyrimidine derivatives play an important role of bioactive compounds, such as antifungal [9, 10], antibacterial [11, 12], acaricidal [13, 14] insecticidal [15, 16], herbicidal [17, 18], and antiviral [19, 20] activities. Our early work has reported a series of novel benzamide derivatives containing a pyrimidine moiety (Figure 1) with better antiviral, insecticidal, antifungal, and antibacterial activities [26,27,28,29,30,31,32,33]
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