Abstract
In this study, thirteen new pyridylpyrazolamide derivatives containing pyrimidine motifs were synthesized via six-step reactions. Bioassay results showed that some of the synthesized compounds revealed good antifungal properties against Sclerotinia sclerotiorum, Phytophthora infestans, Thanatephorus cucumeris, Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica, Botryosphaeria dothidea, and Phompsis sp. at 50 μg/mL, which were similar to those of Kresoxim-methyl or Pyrimethanil. Meanwhile, bioassay results indicated that the synthesized compounds showed a certain insecticidal activity against Spodoptera litura, Mythimna separata, Pyrausta nubilalis, Tetranychus urticae, Rhopalosiphum maidis, and Nilaparvata lugens at 200 μg/mL, which was lower than that of Chlorantraniliprole. To the best of our knowledge, this study is the first report on the antifungal and insecticidal activities of pyridylpyrazol amide derivatives containing a pyrimidine moiety.
Highlights
Plant fungal and insect diseases have posed serious threats to crops in the world and caused a severe loss throughout the world (Strange and Scott, 2005; Yang et al, 2015)
Compounds 6a−6m As shown in Scheme 1, oxalyl chloride (2 mL) and 4 drops of N, N-dimethylformamide (DMF) were added to a mixture of intermediate 5 dissolved in 10 mL CH2Cl2, and reacted at room temperature
In this study, using 2,3-dichloropyridine as the starting material, the title compounds 6a–6m were synthesized in six steps, including hydrazidation, cyclization, bromination or chlorination, oxidation, hydrolyzation, and condensation
Summary
Plant fungal and insect diseases have posed serious threats to crops in the world and caused a severe loss throughout the world (Strange and Scott, 2005; Yang et al, 2015). Some of the available traditional fungicides and insecticides, such as Kresoxim-methyl, Pyrimethanil, Chlorantraniliprole, etc., are widely used to prevent plant harmful fungal and insect diseases. Some of the pyrimidine derivatives (for example, Mepanipyrim, Pyrimethanil, Diflumetorim, Azoxystrobin, and so on), which were known for their abilities to control severe fungal diseases, have been marketed as commercial pesticides worldwide. In our preliminary work, several series of pyrimidine derivatives containing 1,3,4-oxadiazole
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