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.
Expanding the Chemical Space of Succinate Dehydrogenase Inhibitors via the Carbon-Silicon Switch Strategy
Wei, Ge,Huang, Ming-Wei,Wang, Wen-Jie,Wu, Yuan,Mei, Shu-Fen,Zhou, Li-Ming,Mei, Long-Can,Zhu, Xiao-Lei,Yang, Guang-Fu
, p. 3965 - 3971 (2021/05/04)
The carbon-silicon switch strategy has become a key technique for structural optimization of drugs to widen the chemical space, increase drug activity against targeted proteins, and generate novel and patentable lead compounds. Flubeneteram, targeting succinate dehydrogenase (SDH), is a promising fungicide candidate recently developed in China. We describe the synthesis of novel SDH inhibitors with enhanced fungicidal activity to enlarge the chemical space of flubeneteram by employing the C-Si switch strategy. Several of the thus formed flubeneteram-silyl derivatives exhibited improved fungicidal activity against porcine SDH compared with the lead compound flubeneteram and the positive controls. Disease control experiments conducted in a greenhouse showed that trimethyl-silyl-substituted compound W2 showed comparable and even higher fungicidal activities compared to benzovindiflupyr and flubeneteram, respectively, even with a low concentration of 0.19 mg/L for soybean rust control. Furthermore, compound W2 encouragingly performed slightly better control than azoxystrobin and was less active than benzovindiflupyr at the concentration of 100 mg/L against soybean rust in field trials. The computational results showed that the silyl-substituted phenyl moiety in W2 could form strong van der Waals (VDW) interactions with SDH. Our results indicate that the C-Si switch strategy is an effective method for the development of novel SDH inhibitors.
ASK1 INHIBITING AGENTS
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Page/Page column 93, (2020/03/05)
Provided are compounds of Formula (I): Formula (I), including compounds of Formulas (II), (III), (IV), (V) and (VI), wherein X, R1, R2, R3, R4 and n are as defined herein,and pharmaceutically acceptable salts thereof, and methods for their use and production. These compounds can be useful, e.g., in the treatment of disorders responsive to the inhibition of apoptosis signal-regulating kinase 1 (ASK1).
Process for preparing 2- polyhaloacetyl -3- alkoxyacrylates (by machine translation)
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Paragraph 0030-0054, (2020/05/30)
The invention discloses a preparation method 2 - of, polyhalogenated acetyl - 3 3-alkoxy acrylate, wherein the compound II with the chemical structural formula, is dissolved in an organic solvent, for, times and then is heated to I for a certain time . to generate first polyhaloacetyl - 3 3-alkoxyacrylic acid ester, with the chemical structural formula 0.5 - 4h, after reaction for a certain period of time. 0 - 50 °C, The preparation method of the, invention is reasonable second operation and . atomic economical efficiency III, in an 2 -phase reaction, reaction with an acid-binding agent to react for a certain time. (by machine translation)
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.
Synthesis and biological activity of acyl thiourea containing difluoromethyl pyrazole motif
Min, Li-Jing,Zhai, Zhi-Wen,Shi, Yan-Xia,Han, Liang,Tan, Cheng-Xia,Weng, Jian-Quan,Li, Bao-Ju,Zhang, Yong-Gang,Liu, Xing-Hai
, p. 22 - 28 (2019/07/12)
A series of new acyl thiourea derivatives containing difluoromethyl pyrazole moiety were designed and synthesized. Their structures were confirmed by 1H NMR, 31C NMR, MS and HRMS. The bioassay results showed that some of title compounds exhibited good in vivo fungicidal activity against Botrytis cinerea and Fusarium oxysporum and good antibacterial activity against Pseudomonas syringae pv. Lachrymans at 50 mg/L respectively.
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.
Heterocycle-containing two fragrant amines pyrazoles carboxamides and preparation method and application thereof (by machine translation)
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Paragraph 0079; 0080; 0081, (2019/02/04)
The present invention provides a kind of formula (I) indicated by the heterocycle-containing two fragrant amines pyrazoles carboxamides and its preparation method and application, this compound to the agricultural, civil and animal in the technical field of the imago harmful mite and insects, nit and egg demonstrate high insecticidal activity, while at the same time the compound exhibits a good bactericidal activity; (by machine translation)
CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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Paragraph 0126; 0127; 0128, (2019/07/03)
PROBLEM TO BE SOLVED: To provide a cyclic amine compound that has insecticidal activity and/or acaricidal activity, has excellent safety, and can be synthesized in an industrially advantageous manner, and a pest control agent containing the same as an active ingredient. SOLUTION: The present invention provides a compound represented by formula (I), or a salt thereof. (Q is halogeno or the like; R1 is cyano or the like; R2 is H, halogeno or the like; R3 is halogeno, C1-6 alkyl or the like; A is O or S; p1 and p2 are 0 or 1; X1 is halogeno, C1-6 alkoxy or the like; m is an integer of 0-4; X2 is H, a halogeno group or the like; Y is C6-10 aryl or the like; X1 and X2 may form oxymethylene oxy groups). SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
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Paragraph 0415-0418, (2019/07/10)
A compound represented by a formula (I), or a salt thereof: wherein Ar1 is a substituted or unsubstituted C6-10 aryl group, or the like; the number of X1 groups that can be substituted on Ar1 is 5 or less; Xsup
