- Design, synthesis, and insecticidal activity of novel isoxazole derivatives containing bisamide moiety
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In this study, a total of 31 novel isoxazole derivatives containing bisamide moiety were synthesized and evaluated for their insecticidal activity against Plutella xylostella (P. xylostella). Bioassays indicated that some of the target compounds exhibited good insecticidal activity against P. xylostella. In particular, compound E26 revealed excellent insecticidal activity against P. xylostella, with a 50% lethal concentration (LC50) value of 4.6 μg/mL, which was even better than those of chlorpyrifos (7.7 μg/mL), beta-cypermethrin (12.8 μg/mL), and azadirachtin (10.2 μg/mL). These results indicated that isoxazole derivatives containing bisamide moiety could be developed as novel and promising insecticides. To the best of our knowledge, it is the first report on the insecticidal activity of this series of novel isoxazole derivatives containing bisamide moiety.
- Yang, Zaibo,Zhao, Yang,Li, Pei,He, Yinju
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- Novel pyrazole-hydrazone derivatives containing an isoxazole moiety: Design, synthesis, and antiviral activity
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In this study, a series of novel pyrazole-hydrazone derivatives containing an isoxazole moiety were synthesized. Antiviral bioassays indicated that some of the title compounds exhibited better in vivo antiviral activities against tobacco mosaic virus (TMV). In particular, compounds 6a, 6c and 6q exhibited the best curative activity, protection activity, and inactivation activity against TMV, respectively, which were superior to those of Ningnanmycin. This study demonstrated that this series of novel pyrazole-hydrazone derivatives containing an isoxazole amide moiety could effectively control TMV.
- Yang, Zaibo,Li, Pei,Gan, Xiuhai
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- 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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p. 164 - 167
(2017/11/20)
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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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- 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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- NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS
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A compound of the following Formula (I) is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with -N, -O, or -S adjacent to the -Ar substituent or adjacent to the point of attachment for the -Ar substituent; Ar is aryl or heteroaryl; R is -CH3, -CH2F, -CHF2 or -CH=CH2; V is -H, -CH3 or =0; W is -NO2, -CI, -Br, -CH2OH, or -CN; X is -CI, -Br, -F, -CH3, -OCH3, or -CN; Y is -CH or -N; and Z is -CH or -N. This compound is useful in compositions for the prevention and treatment of influenza virus.
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Page/Page column 53
(2012/04/17)
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- SUBSTITUTED AZOLE AROMATIC HETEROCYCLES AS INHIBITORS OF 11BETA-HSD-1
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Compounds of formula I and IV are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorder: wherein the variables A-B, R1, R2, m, and Q are described herein.
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Page/Page column 55
(2008/06/13)
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- 2,3-Lower alkylenepenam-3-carboxylic acid derivatives and processes for the preparation thereof
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A process for the preparation of SPC1 Which comprises reacting SPC2 With a base, wherein Y is a residue of an acid, wherein R1 is amino, (halophenylimino-1-lower alkanoylthiomethyl)amino or acylamino and wherein R2 is carboxy or a protected carboxy, R3 is lower alkyl, R4 is lower alkylene and X is --S-- or EQU1
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