176969-33-8Relevant articles and documents
Synthesis, Nematocidal Activity and Docking Study of Novel Chiral 1-(3-Chloropyridin-2-yl)-3-(difluoromethyl)-1H-pyrazole-4-carboxamide Derivatives
Zhao, Wen,Shen, Zhong-Hua,Xu, Tian-Ming,Peng, Wei-Li,Liu, Xing-Hai
, p. 1751 - 1756 (2017)
A novel series of pyrazole carboxamide derivatives had been designed, synthesized and some of them exhibited good nematocidal activity.
CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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Paragraph 0323-0324, (2020/06/15)
A pest control agent according to the present invention contains a compound of formula (I) (in the formula, Ar represents a substituted or unsubstituted C6-10 aryl group, R1 represents a cyano group or a substituted or unsubstituted thiocarbamoyl group, R2 represents a hydrogen atom, a halogeno group, a substituted or unsubstituted C1-6 alkyl group, a hydroxyl group, or a substituted or unsubstituted C1-6 alkoxy group, R3 represents a hydrogen atom, a halogeno group, a substituted or unsubstituted C1-6 alkyl group, or the like, and Q represents a cyclic amino group) or a salt thereof.
Expedient discovery for novel antifungal leads targeting succinate dehydrogenase: Pyrazole-4-formylhydrazide derivatives bearing a diphenyl ether fragment
Chen, Min,Li, Guohua,Lu, Aimin,Qiu, Lingling,Wang, An,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
, p. 14426 - 14437 (2020/12/22)
The pyrazole-4-carboxamide scaffold containing a flexible amide chain has emerged as the molecular skeleton of highly efficient agricultural fungicides targeting succinate dehydrogenase (SDH). Based on the above vital structural features of succinate dehydrogenase inhibitors (SDHI), three types of novel pyrazole-4-formylhydrazine derivatives bearing a diphenyl ether moiety were rationally conceived under the guidance of a virtual docking comparison between bioactive molecules and SDH. Consistent with the virtual verification results of a molecular docking comparison, the in vitro antifungal bioassays indicated that the skeleton structure of title compounds should be optimized as an N′-(4-phenoxyphenyl)-1H-pyrazole-4-carbohydrazide scaffold. Strikingly, N′-(4-phenoxyphenyl)-1H-pyrazole-4-carbohydrazide derivatives 11o against Rhizoctonia solani, 11m against Fusarium graminearum, and 11g against Botrytis cinerea exhibited excellent antifungal effects, with corresponding EC50 values of 0.14, 0.27, and 0.52 μg/mL, which were obviously better than carbendazim against R. solani (0.34 μg/mL) and F. graminearum (0.57 μg/mL) as well as penthiopyrad against B. cinerea (0.83 μg/mL). The relative studies on an in vivo bioassay against R. solani, bioactive evaluation against SDH, and molecular docking were further explored to ascertain the practical value of compound 11o as a potential fungicide targeting SDH. The present work provided a non-negligible complement for the structural optimization of antifungal leads targeting SDH.
