- Novel 2－ aryloxynicotinamide compound as well as preparation method and application thereof
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The invention relates to a novel 2 - aryloxynicotinamide compound as well as a preparation method and application. of the 2 - aryloxynicotinamide compound as shown in the following formula (I). The compound can be used for preparing,aryloxy nicotinic acid compounds and derivatives thereof through a condensation reaction and a carbon hydrogen bond direct etherification method as shown in the formula shown in the specification. The invention relates to a novel method for preparing. 2 - aryloxynicotinic acid compounds and, derivatives thereof as shown in the structural formula shown. in the structural formula shown in the following formula. In Formula (I), the steric configuration of the carbon atom attached to the substituent R is R or S,Ar, and the aromatic substituent (is shown in more detail in the specification).
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- Design, Synthesis, and Herbicidal Activity of Novel Diphenyl Ether Derivatives Containing Fast Degrading Tetrahydrophthalimide
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To seek new protoporphyrinogen oxidase (PPO) inhibitors with better biological activity, a series of novel diphenyl ether derivatives containing tetrahydrophthalimide were designed based on the principle of substructure splicing and bioisomerization. PPO inhibition experiments exhibited that 6c is the most potential compound, with the half-maximal inhibitory concentration (IC50) value of 0.00667 mg/L, showing 7 times higher activity than Oxyfluorfen (IC50 = 0.0426 mg/L) against maize PPO and similar herbicidal activities to Oxyfluorfen in weeding experiments in greenhouses and field weeding experiments. In view of the inspected bioactivities, the structure-activity relationship (SAR) of this series of compounds was also discussed. Crop selection experiments demonstrate that compound 6c is safe for soybeans, maize, rice, peanuts, and cotton at a dose of 300 g ai/ha. Accumulation analysis experiments showed that the accumulation of 6c in some crops (soybeans, peanuts, and cotton) was significantly lower than Oxyfluorfen. Current work suggests that compound 6c may be developed as a new herbicide candidate in fields.
- Cheng, Yuan,Fu, Ying,Gao, Shuang,Hu, Jia-Jun,Jiang, Mao-Jun,Ren, Tao,Ye, Fei,Zhao, Li-Xia,Zou, Yue-Li
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p. 3729 - 3741
(2020/04/09)
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- NOVEL PHENYL AMIDE OR PYRIDYL AMIDE DERIVATIVES
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This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
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Page/Page column 22
(2010/05/13)
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- Activation and inhibition of kidney CLC-K chloride channels by fenamates
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CLC-K Cl- channels are selectively expressed in kidney and ear, where they are pivotal for salt homeostasis, and loss-offunction mutations of CLC-Kb produce Bartter's syndrome type III. The only ligand known for CLC-K channels is a derivative o
- Liantonio, Antonella,Picollo, Alessandra,Babini, Elena,Carbonara, Giuseppe,Fracchiolla, Giuseppe,Loiodice, Fulvio,Tortorella, Vincenzo,Pusch, Michael,Camerino, Diana Conte
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p. 165 - 173
(2007/10/03)
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- Nicotinamide Ethers: Novel Inhibitors of Calcium-Independent Phosphodiesterase and Rolipram Binding
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The synthesis and biological properties of a series of nicotinamide ethers are described.These compounds, structurally novel calcium-independent phosphodiesterase inhibitors, also inhibit the binding of rolipram to rat brain membranes and reverse rese
- Vinick, Fredric J.,Saccomano, Nicholas A.,Koe, B. Kenneth,Nielsen, Jann A.,Williams, Ian H.,et al.
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- SELECTIVE CLEAVAGE OF THE ETHER AND AMIDE BONDS IN N-(2,4-DIFLUOROPHENYL)-2--3-PYRIDINECARBOXAMIDE (DIFLUFENICAN)
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Heated to reflux in water containing 8 gpercent KOH, the herbicide diflufenican -3-pyridinecarboxamide, 1> was selectively transformed into 2--3-pyridinecarboxylic acid (2) plus 2,4-difluoroaniline (5); after 60 hr of heating, 27percent of the initial diflufenican was transformed, yielding 21percent (molepercent relative to initial diflufenican) of compound 2.Heated to reflux in a mixture of acetic acid + concentrate hydrochloric acid, diflufenican was transformed into a mixture of N-(2,4-difluorophenyl)-2-hydroxy-3-pyridinecarboxamide (3) and 2-hydroxy-3-carboxypyridine (4) plus 2,4-difluoroaniline (5) and 3-trifluoromethylphenol (6); after 48 hr of heating, diflufenican was completely transformed, yielding 28percent (molepercent relative to initial diflufenican) of compound 3, and 57percent of compound 4.The base catalyzed hydrolysis thus selectively yielded compound 2; the acid catalyzed one yielded compounds 3 + 4: diflufenican first was transformed into compound 3, which thereafter was transformed into compound 4.
- Rouchaud, Jean,Gustin, Fabrice,Moulart, Claude,Herin, Marc
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p. 339 - 344
(2007/10/02)
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- N-substituted, 2-phenoxynicotinamide compounds and the herbicidal use thereof
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This invention relates to novel herbicidal compounds having the formula STR1 in which X is chloro, bromo, trifluoromethyl, methyl or ethyl; R1 is hydrogen or C3 -C5 alkenyl; and R2 is (a) C3 -C5
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