- Design, synthesis, and bioevaluation of substituted phenyl isoxazole analogues as herbicide safeners
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Herbicide safeners enhance herbicide detoxification in crops without affecting target weed sensitivity. To enhance crop tolerance to the toxicity-related stress caused by the herbicide acetochlor (ACT), a new class of substituted phenyl isoxazole derivatives was designed by an intermediate derivatization method as herbicide safeners. Microwave-assisted synthesis was used to prepare the phenyl isoxazole analogues, and all of the structures were confirmed via IR, 1H NMR, 13C NMR, and HRMS. Compound I-1 was further characterized by X-ray diffraction analysis. Bioassay results showed that most of the obtained compounds provided varying degrees of safening against ACT-induced injury by increasing the corn growth recovery, glutathione content, and glutathione S-transferase activity. In particular, compound I-20 showed excellent safener activity against ACT toxicity, comparable to that of the commercial safener benoxacor. Gaussian calculations have been performed and the results indicated that the nucleophilic ability of compound I-20 is higher than that of benoxacor, thus the activity is higher than that of benoxacor. These findings demonstrate that phenyl isoxazole derivatives possess great potential for protective management in cornfields.
- Fu, Ying,Gao, Shuang,Gao, Ying-Chao,Guo, Ke-Liang,Li, Juan-Juan,Wang, Zi-Wei,Ye, Fei,Zhao, Li-Xia
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p. 10550 - 10559
(2020/11/05)
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- Synthesis and biological activity of ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylate
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A series of novel ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylates I-1-6 were synthesized. The structures of all target compounds were characterized by 1H NMR, 13C NMR, IR,MS and elemental analyses. Their fungicidal and herbicidal activities were evaluated. The results of preliminary bioassays show that the title compounds I-4 possess 20-50% inhibition against most of the tested plants at the dosage of 150 g ai/ha, while the title compounds I-1-5 possess 32-58% inhibition against FusaHum graminearum, Thanatephorus cucumeris, Botrytis cinereapers and Fusarium oxysporum in vitro at the concentration of 100 mg/L.
- Wang, Wei,Wang, Lie-Ping,Mao, Min-Zhen,Zhang, Xiao-Guang,Zheng, Xiao-Rui,Huang, Xiao-Ying,Xue, Chao,Ning, Bin-Ke
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supporting information
p. 164 - 167
(2017/11/20)
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- PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF
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Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient.
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Paragraph 0105; 0106; 0107; 0108
(2014/02/16)
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- IMPROVED PROCESS FOR PREPARING PENICILLINS AND INTERMEDIATE COMPOUNDS
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Disclosed is an improved process for the preparation of isoxazolyl penicillins of formula (I), wherein X1 and X2 can be independently selected from the group comprising hydrogen, chlorine or fluorine, and its pharmaceutically suitable salts. The process is economic in -situ synthetic method without isolation of any intermediate. (I).
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Page/Page column 9-10
(2013/02/27)
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- Synthesis of 1,2,3-triazole substituted isoxazoles via copper (I) catalyzed cycloaddition
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The synthesis of a series of 3,5-disubstituted isoxazole-4-carboxylic esters containing N-substituted 1,2,3-triazoles (V) starting from various benzaldehydes (I) is reported. Benzaldehydes undergo oximation with hydroxylamine hydrosulfate. Later, chlorination followed by condensation with methylacetoacetate and the hydrolysis of the resulting ester afforded respective carboxylic acid (II), which on chlorination with PCl5 gave the corresponding acid chlorides (III). The coraboxylic acid chlorides (III) on propargylation gave propargylic esters (IV) and these on click reaction gave the title compounds (V).
- Ramana, P. Venkata,Reddy, A. Ram
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p. 621 - 627
(2012/09/07)
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- Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists
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A series of isoxazole carboxamide derivatives has been developed as potent ghrelin receptor antagonists. The synthesis and structure-activity relationship (SAR) are described.
- Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Liu, Bo,Schaefer, Verlyn G.,Falls, Douglas H.,Kaszubska, Wiweka,Colins, Christine A.,Sham, Hing L.,Liu, Gang
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p. 1201 - 1204
(2007/10/03)
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