149978-43-8Relevant articles and documents
Synthesis and Biological Activity of Novel Pyrazol-5-yl-benzamide Derivatives as Potential Succinate Dehydrogenase Inhibitors
Wang, Wei,Wang, Jianhua,Wu, Furan,Zhou, Huan,Xu, Dan,Xu, Gong
, p. 5746 - 5754 (2021/05/26)
To promote the discovery and development of new fungicides, a series of novel pyrazol-5-yl-benzamide derivatives were designed, synthesized by hopping and inversion of amide groups of pyrazole-4-carboxamides, and evaluated for their antifungal activities. The bioassay data revealed that compound 5IIc exhibited an excellent in vitro activity against Sclerotinia sclerotiorum with an EC50 value of 0.20 mg/L, close to that of commercial fungicide Fluxapyroxad (EC50 = 0.12 mg/L) and Boscalid (EC50 = 0.11 mg/L). For Valsa mali, compound 5IIc (EC50 = 3.68 mg/L) showed a significantly higher activity than Fluxapyroxad (EC50 = 12.67 mg/L) and Boscalid (EC50 = 14.83 mg/L). In addition, in vivo experiments proved that compound 5IIc has an excellent protective fungicidal activity with an inhibitory rate of 97.1% against S. sclerotiorum at 50 mg/L, while the positive control Fluxapyroxad showed a 98.6% inhibitory effect. The molecular docking simulation revealed that compound 5IIc interact with TRP173, SER39, and ARG43 of succinate dehydrogenase (SDH) through a hydrogen bond and p-πinteraction, which could explain the probable mechanism of the action between compound 5IIc and target protein. Also, the SDH enzymatic inhibition assay was carried out to further validate its mode of action. These results demonstrate that compound 5IIc could be a promising fungicide candidate and provide a valuable reference for further investigation.
Fluorine-containing pyrazole amide derivative, and preparation method and application thereof
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Paragraph 0073; 0077-0078, (2020/06/09)
The invention discloses a fluorine-containing pyrazole amide derivative, and a preparation method and application thereof. The structural formula of the fluorine-containing pyrazole amide derivative is as described in the invention. In the structural formula, R1 is a trifluoromethyl or difluoromethyl group; R2 is hydrogen, chlorine, fluorine, bromine or iodine; and R3 is polysubstituted benzene orpolysubstituted pyridine. The fluorine-containing pyrazole amide derivative has remarkable antifungal activity and can provide a basis for development of a novel bactericide with the fluorine-containing pyrazole amide compound derivative as an active ingredient.
PYRIDAZINONE GLUCOKINASE ACTIVATORS
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Page/Page column 44, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.