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

Wu Zhibing | Zendy; Yang Guangqian | Zendy; Zhao Xin | Zendy; Wu Jiangchun | Zendy; Wu Shixi | Zendy

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

Author(s) -

Wu Zhibing,

Yang Guangqian,

Zhao Xin,

Wu Jiangchun,

Wu Shixi

Publication year - 2019

Publication title -

journal of heterocyclic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.321

H-Index - 59

eISSN - 1943-5193

pISSN - 0022-152X

DOI - 10.1002/jhet.3400

Subject(s) - botrytis cinerea , gibberella zeae , fusarium oxysporum , sclerotinia sclerotiorum , chemistry , trifluoromethyl , antifungal , carboxamide , bioassay , phytophthora infestans , stereochemistry , fusarium , horticulture , microbiology and biotechnology , organic chemistry , biology , biochemistry , alkyl , genetics , gene

A series of 1‐(3‐chloropyridin‐2‐yl)‐5‐(trifluoromethyl)‐1 H ‐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 T 3 (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 T 3 (>200, >200, and >200 μg/mL); the EC 50 values of 7d and 7c against B. cinerea were 94.9 and 56.2 μg/mL, respectively. The EC 50 values of 7a , 7d , and 7c against S. sclerotiorum were 73.5, 78.7, and 68.5 μg/mL, respectively.

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