Design, Synthesis and Antifungal Evaluation of N‐Substituted‐1‐(3‐chloropyridin‐2‐yl)‐N‐(pyridin‐4‐yl)‐5‐(trifluoromethyl)‐1H‐pyrazole‐4‐carboxamide Derivatives

A series of 1‐(3‐chloropyridin‐2‐yl)‐5‐(trifluoromethyl)‐1H‐pyrazole‐4‐carboxamide derivatives which have di‐substituents on nitrogen were designed and synthesized. Bioassay results showed that all the synthetic compounds exhibited lower antifungal activities against Gibberella zeae, Cytospora mands...

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Veröffentlicht in:Journal of heterocyclic chemistry 2019-01, Vol.56 (1), p.234-238
Hauptverfasser: Wu, Zhibing, Yang, Guangqian, Zhao, Xin, Wu, Jiangchun, Wu, Shixi
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Sprache:eng
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Zusammenfassung:A series of 1‐(3‐chloropyridin‐2‐yl)‐5‐(trifluoromethyl)‐1H‐pyrazole‐4‐carboxamide derivatives which have di‐substituents on nitrogen were designed and synthesized. Bioassay results showed that all the synthetic compounds exhibited lower antifungal activities against Gibberella zeae, Cytospora mandshurica, and Fusarium oxysporum than T3 (14.7, 21.1, and 32.7 μg/mL), but some of them exhibited better activities against Botrytis cinerea, Phytophthora infestans, and Sclerotinia sclerotiorum than T3 (>200, >200, and >200 μg/mL); the EC50 values of 7d and 7c against B. cinerea were 94.9 and 56.2 μg/mL, respectively. The EC50 values of 7a, 7d, and 7c against S. sclerotiorum were 73.5, 78.7, and 68.5 μg/mL, respectively.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3400