40926-73-6Relevant academic research and scientific papers
Design and Synthesis of Novel 4-Hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one Derivatives for Use as Herbicides and Evaluation of Their Mode of Action
Lei, Kang,Li, Pan,Yang, Xue-Fang,Wang, Shi-Ben,Wang, Xue-Kun,Hua, Xue-Wen,Sun, Bin,Ji, Lu-Sha,Xu, Xiao-Hua
, p. 10489 - 10497 (2019/10/02)
In order to develop a novel herbicide containing the β-triketone motif, a series of 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one derivatives were designed and synthesized. The bioassay results showed that compound II15 had good pre-emergent herbicidal activity even at a dosage of 187.5 g ha-1. Moreover, compound II15 showed a broader spectrum of weed control when compared with a commercial herbicide 2,4-dichlorophenoxyacetic acid (2,4-D), and displayed good crop safety to Triticum aestivum L. and Zea mays Linn. when applied at 375 g ha-1 under pre-emergence conditions, which indicated its great potential as a herbicide. More importantly, studying the molecular mode of action of compound II15 revealed that the novel triketone structure is a proherbicide of its corresponding phenoxyacetic acid auxin herbicide, which has a herbicidal mechanism similar to that of 2,4-D. The present work indicates that the 4-hydroxyl-3-(2-phenoxyacetyl)-pyran-2-one motif may be a potential lead structure for further development of novel auxin-type herbicides.
Carboxy Group as a Remote and Selective Chelating Group for C?H Activation of Arenes
Li, Shangda,Wang, Hang,Weng, Yunxiang,Li, Gang
supporting information, p. 18502 - 18507 (2019/11/14)
The first example of carboxy group assisted, remote-selective C(sp2)?H activation with a PdII catalyst has been developed and proceeds through a possible κ2 coordination of the carboxy group, thus suppressing the ortho-C?H activation through κ1 coordination. Besides meta-C?H olefination, direct meta-arylation of hydrocinnamic acid derivatives with low-cost aryl iodides has been achieved for the first time. These findings may motivate the exploration of novel reactivities of the carboxy assisted C?H activation reactions with intriguing selectivities.
Isoflavone amide derivatives, their preparation method and medical use
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Paragraph 0095, (2017/08/31)
The invention belongs to the field of medicinal chemistry, and relates to derivatives of isoflavones amides, as well as a preparation method and medical application of derivatives, in particular to the derivatives of the isoflavones amides with the general formula of (I) shown as the specification, the preparation method and the medical application of the derivatives, particularly the application of the derivatives of the isoflavones amides serving as medicaments for preventing or treating hyperlipemia, adiposis or type-II diabetes.
Synthesis and biological evaluation of aryloxyacetamide derivatives as neuroprotective agents
Zhong, Yan,Xu, Yi,Zhang, Ai-Xia,Li, Xiao-Feng,Xu, Zhao-Ying,Li, Ping,Wu, Bin
supporting information, p. 2526 - 2530 (2016/07/07)
A series of new aryloxyacetamide derivatives 10a-s and 14a-m are designed and synthesized. Their protective activities against the glutamate-induced cell death were investigated in differentiated rat pheochromocytoma cells (PC12 cells). Most compounds exhibited neuroprotective effects, especially for 10m, 10r, 14b and 14c, which showed potential protection of PC12 cells at three doses (0.1, 1.0, 10 μM). MTT assay, Hoechst 33342/PI double staining, and high content screening (HCS) revealed that pretreatment of the cells with 10m, 10r, 14b and 14c has significantly decreased the extent of cell apoptosis in a dose-dependent manner. The results of western blot analysis demonstrated these compounds suppressed apoptosis of glutamate-induced PC12 cells via caspase-3 pathway. These compounds can be lead compounds for further discovery of neuroprotective agents for treating cerebral ischemic stroke. Basic structure-activity relationships are also presented.
Formononetin derivatives and preparation methods and medical application thereof
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Paragraph 0087; 0088; 0089; 0099; 0100; 0101, (2017/04/29)
The invention relates to the field of pharmaceutical chemistry, and relates to formononetin derivatives and preparation methods and medical application thereof, in particular to formononetin derivatives with the general formula as shown in (I), preparation methods thereof, pharmaceutical compositions containing the compounds and medical application of the derivatives and the pharmaceutical compositions, particularly, application of the derivatives and the pharmaceutical compositions serving as drugs for preventing or treating hyperlipidaemia or obesity or type-II diabetes. Please see the formula in the description.
Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities
Wang, Wenbin,He, Yi,Xu, Pei,You, Qidong,Xiao, Hong,Xiang, Hua
, p. 4428 - 4433 (2015/08/03)
A series of isoflavone amides were designed with isoflavone in place of the scaffold of 2-arylbenzoxazole as cholesterol ester transfer protein (CETP) inhibitors. Twelve new compounds were synthesized, and their inhibitory activities of CETP and preadipocyte proliferation were assayed. The hypolipidemic potency of the most effective compound HY-2c was further tested in vivo by hamster. The results indicate that HY-2c exhibited favorable antihyperlipidemic and preadipocyte antiproliferative activities.
Preparation of diastereomerically pure dilignol model compounds
Buendia, Julien,Mottweiler, Jakob,Bolm, Carsten
supporting information; experimental part, p. 13877 - 13882 (2012/01/15)
A gram-scale synthetic access to diastereomerically pure dilignol β-O-4 type model compounds, which represent valuable candidates for studies of lignin cleavage and valorization, is described. Following a straightforward procedure both diastereoisomers of 1,3-dilignols can be prepared. In the key-step, tert-butyl aryloxy esters are used as enolate precursors for additions on aldehydes. After separation, the resulting erythro and threo β-hydroxy esters are independently reduced to afford the target compounds in high yields.
Aryloxyacetic esters structurally related to α-Asarone as potential antifungal agents
Jimenez, Fabiola,Cruz, Maria Del Carmen,Zuniga, Clara,Martinez, Maria A.,Chamorro, German,Diaz, Francisco,Tamariz, Joaquin
experimental part, p. 33 - 57 (2010/10/20)
A series of aryloxyacetic ester analogues 8-13 was synthesized based on the potential pharmacophores of the antifungal agents α-Asarone (1) and 2-5. Their antifungal activity was tested in vitro for their growth inhibitory activities against pathogenic fungi. The in vitro antifungal evaluation of these alkyl and aryl esters shows that derivatives 10 displayed the highest antifungal and fungicidal activities against Cryptococcus neoformans and C. gattii. These results support the idea that the phenoxyacetic frame is a potent pharmacophore for the design of potential antifungal drugs. Graphical Abstract: [Figure not available: see fulltext.]
Design, synthesis and in vitro antibacterial/antifungal evaluation of novel 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid derivatives
Yu, Zhiyi,Shi, Guanying,Sun, Qiu,Jin, Hong,Teng, Yun,Tao, Ke,Zhou, Guoping,Liu, Wei,Wen, Fang,Hou, Taiping
experimental part, p. 4726 - 4733 (2010/01/06)
A series of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7(1-piperazinyl)quinoline-3-carboxylic acid (norfloxacin) derivatives were prepared according to the principle of combinating bioactive substructures and tested for their activities against five plant pathogenic bacteria and three fungi in vitro. The preliminary bioassays indicated that almost all synthesized target compounds retained the antibacterial activities of norfloxacin and had some antifungal activities as carboxylic acid amide compounds. The activities of compounds 1 and 22 against Xanthomonas oryzae were better than norfloxacin and all tested compounds had better antibacterial activities as compared to the agricultural streptomycin sulfate (a commercial bactericide) against X. oryzae, Xanthomonas axonopodis and Erwinia aroideae. Additionally, compounds 2 and 20 displayed good antifungal activities against Rhizoctonia solani and their inhibition of growth reached 83% and 94% respectively at the concentration of 200 mg/L.
SYNTHESIS OF NEW N-ACYL DERIVATIVES OF DL-TRANS-1,2-AMINOCYCLOHEXANOL
Pekala, Elzbieta,Gajewczyk, Leonard,Marona, Henryk
, p. 339 - 342 (2007/10/02)
New amide derivatives of Dl-trans-1,2-aminocyclohexanol, with a potential action on the cardiovascular system, were obtained.Keywords: N-acyl derivatives of DL-trans-1,2-aminocyclohexanol, elemental analysis, 1H NMR.
