1261737-05-6Relevant articles and documents
Design, Synthesis, and Pesticidal Activities of Pyrimidin-4-amine Derivatives Bearing a 5-(Trifluoromethyl)-1,2,4-oxadiazole Moiety
Cheng, Long,Liu, Xing-Hai,Wen, Yong-Hui,Wu, Ning-Jie,Xu, Tian-Ming
, p. 6968 - 6980 (2021)
It is important to discover new pesticides with new modes of action because of the increasing evolution of pesticide resistance. In this study, a series of novel pyrimidin-4-amine derivatives containing a 5-(trifluoromethyl)-1,2,4-oxadiazole moiety were designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, and HRMS. Bioassays indicated that the 29 compounds synthesized possessed excellent insecticidal activity against Mythimna separata, Aphis medicagini, and Tetranychus cinnabarinus and fungicidal activity against Pseudoperonospora cubensis. Among these pyrimidin-4-amine compounds, 5-chloro-N-(2-fluoro-4-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzyl)-6-(1-fluoroethyl)pyrimidin-4-amine (U7) and 5-bromo-N-(2-fluoro-4-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzyl)-6-(1-fluoroethyl) pyrimidin-4-amine(U8) had broad-spectrum insecticidal and fungicidal activity. The LC50 values were 3.57 ± 0.42, 4.22 ± 0.47, and 3.14 ± 0.73 mg/L for U7, U8, and flufenerim against M. separata, respectively. The EC50 values were 24.94 ± 2.13, 30.79 ± 2.21, and 3.18 ± 0.21 mg/L for U7, U8, and azoxystrobin against P. cubensis, respectively. The AChE enzymatic activity testing revealed that the enzyme activities of compounds U7, U8, and flufenerim are 0.215, 0.184, and 0.184 U/mg prot, respectively. The molecular docking results of compounds U7, U8, and flufenerim with the AChE model demonstrated the opposite docking mode between compound U7 or U8 and positive control flufenerim in the active site of AChE. The structure-activity relationships are also discussed. This work provided excellent pesticide for further optimization. Density functional theory analysis can potentially be used to design more active compounds.
AMINO ACID COMPOUNDS WITH UNBRANCHED LINKERS AND METHODS OF USE
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Paragraph 00271; 00272, (2020/01/24)
The invention relates to compounds of formula (A): or a salt thereof, wherein R1, R2, R5a, R5b, R6a, R6b, R7a, R7b, R8a, R8b, R9a, R9b, R10a, R10b, R11a, R11b, R21, n, and G are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are ανβ6 integrin inhibitors that are useful for treating fibrosis such, as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
INDOLE AND AZAINDOLE MODULATORS OF THE ALPHA 7 NACHR
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Page/Page column 47, (2011/05/05)
This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a pharmaceutically acceptable salt thereof.
PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL
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Page/Page column 151; 152, (2010/12/18)
A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.