- Synthesis, nematicidal activity and docking study of novel chromone derivatives containing substituted pyrazole
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A series of chromone derivatives containing substituted pyrazole were designed and synthesized. Preliminary bioassays showed that most of the synthesized compounds exhibited good nematicidal activity in vivo against Meloidogyne incognita at 10 mg/L. Among the tested compounds, A10 and A11 exhibited 100% inhibition rates. In addition, the molecular docking results indicated that both compound A10 and A11 interacts with amino acid residue Tyr121, Trp279, Tyr70, Trp84 and Phe330 of AChE via hydrogen bond and π–π stacking. This investigation suggested that the chromone containing substituted pyrazole scaffold could be further optimized to explore novel, high-bioactivity nematicidal leads.
- Li, Wei,Li, Jiuhui,Shen, Hongfeng,Cheng, Jiagao,Li, Zhong,Xu, Xiaoyong
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supporting information
p. 911 - 914
(2017/11/01)
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- New strategy for the regioselective synthesis of 1-phenyl-3- trifluoromethyl-1H-pyrazoles
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A regioselective synthesis of 3-trifluoromethyl-1-phenyl-1H-pyrazoles (1,3-isomers) as well as their 1,5-isomers (5-trifluoromethyl-1-phenyl-1H- pyrazoles), is described. The 1,3-isomers were obtained from the reaction of 4-alkoxy-1,1,1-trifluoroalk-3-en-2-ones with arylhydrazones followed by deprotective hydrolysis while the 1,5-isomer was obtained by direct cyclocondensation of 4-alkoxy-1,1,1-trifluoroalk-3-en-2-ones with phenylhydrazine. An unequivocal assignment of the 1,3- and 1,5-isomers of the pyrazole products is given.
- Zanatta, Nilo,Amaral, Simone S.,Dos Santos, Josiane M.,Da Silva, Andréia M.P.W.,Schneider, Juliana M.F.M.,Fernandes, Liana Da S.,Bonacorso, Helio G.,Martins, Marcos A.P.
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p. 4076 - 4079
(2013/07/25)
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- New one-pot, efficient, and regioselective method for the synthesis of 3-Trifluoromethyl-1H-1-phenylpyrazoles and alkyl 3-carboxylate analogs
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An efficient and regioselective procedure for the synthesis of a series of alkyl(aryl/heteroaryl) substituted 3-trifluoromethyl-1H-1-phenylpyrazoles and alkyl 3-carboxylate analogs, from the cyclocondensation reactions of 4-alkoxy-1,1,1-trihaloalk-3-en-2-ones [CX3C(O)CR2=CR 1(OMe/OEt), where R1 = H, Me, Ph, 2-Furyl; R2 = H; R1-R2 = -C4H8- and X = F, Cl] and 1-phenylsemicarbazide in an acidified alcoholic medium (R 3OH/H2SO4), where R3 = Me, Et, Pri was successfully applied and is described here in detail. 2012 Elsevier Ltd. All rights reserved.
- Bonacorso, Helio G.,Correa, Michele S.,Porte, Liliane M.F.,Pittaluga, Everton P.,Zanatta, Nilo,Martins, Marcos A.P.
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p. 5488 - 5491
(2012/11/07)
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- PYRAZOLE DERIVATIVES AS MODULATORS OF CALCIUM RELEASE -ACTIVATED CALCIUM CHANNEL
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Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
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Page/Page column 59
(2011/04/26)
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- Regioselective synthesis of trifluoromethyl group substituted pyrazole derivatives from 1-aryl-3,4,4,4-tetrafluoro-2-buten-1-ones
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Trifluoromethyl group substituted pyrazole derivatives were prepared from hydrazines and 1-aryl-3,4,4,4-tetrafluoro-2-buten-1-ones obtained by the deoxyfluorination of β-diketones. The reaction proceeded regioselectively and 5-aryl-3-trifluoromethyl-1-phe
- Sano, Keisuke,Hara, Shoji
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experimental part
p. 349 - 357
(2010/04/27)
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- Improved regioselectivity in pyrazole formation through the use of fluorinated alcohols as solvents: Synthesis and biological activity of fluorinated tebufenpyrad analogs
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(Chemical Equation Presented) The preparation of N-methylpyrazoles is usually accomplished through reaction of a suitable 1,3-diketone with methylhydrazine in ethanol as the solvent. This strategy, however, leads to the formation of regioisomeric mixtures of N-methylpyrazoles, which sometimes are difficult to separate. We have determined that the use of fluorinated alcohols such as 2,2,2-trifluoroethanol (TFE) and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) as solvents dramatically increases the regioselectivity in the pyrazole formation, and we have used this modification in a straightforward synthesis of fluorinated analogs of Tebufenpyrad with acaricide activity.
- Fustero, Santos,Roman, Raquel,Sanz-Cervera, Juan F.,Simon-Fuentes, Antonio,Cunat, Ana C.,Villanova, Salvador,Murguia, Marcelo
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p. 3523 - 3529
(2008/09/20)
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- HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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A hydrazide compound represented by the formula (1): has excellent pesticidal activity.
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Page/Page column 526
(2008/06/13)
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- Insecticidal anthranilic diamides: A new class of potent ryanodine receptor activators
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A novel class of anthranilic diamides has been discovered with exceptional insecticidal activity on a range of Lepidoptera. These compounds have been found to exhibit their action by release of intracellular Ca2+ stores mediated by the ryanodine receptor. The discovery, synthesis, structure-activity, and biological results are presented.
- Lahm, George P.,Selby, Thomas P.,Freudenberger, John H.,Stevenson, Thomas M.,Myers, Brian J.,Seburyamo, Gilles,Smith, Ben K.,Flexner, Lindsey,Clark, Christopher E.,Cordova, Daniel
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p. 4898 - 4906
(2007/10/03)
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- Haloacetylated enol ethers, 19: Synthesis of 3-(2-thienyl)- and 3-(2-furyl)-5-trihalomethyl substituted azoles
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Heterocyclization of 1,1,1-trifluoro[chloro]-4-methoxy-4-[2-tienyl]-3- buten-2-one and 1,1,1-trifluoro[chloro]-4-methoxy-4-[2-furyl]-3-buten-2-ones into isoxazoles and pyrazoles derivatives as a new type of trihalomethylated bicyclic heterocycles is reported. Georg Thieme Verlag Stuttgart.
- Flores, Alex F. C.,Brondani, Sergio,Pizzuti, Lucas,Martins, Marcos A. P.,Zanatta, Nilo,Bonacorso, Helio G.,Flores, Darlene C.
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p. 2744 - 2750
(2007/10/03)
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- Synthesis of fluorinated heterocycles
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Selected 1,3-diketones having a trifluoromethyl group and/or a fluorine in the 2-position were condensed with aromatic hydrazines, hydroxylamine, urea, thiourea, guanidine, and substituted anilines producing pyrazoles, isoxazoles, pyrimidines, and quinolines, respectively, in yields ranging from 27 to 87%.
- Sloop, Joseph C.,Bumgardner, Carl L.,Loehle, W. David
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p. 135 - 147
(2007/10/03)
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