- Triketone compound containing quinoxaline structure, and preparation method and application thereof
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The invention belongs to the technical field of medicine synthesis, and particularly relates to a triketone compound containing a quinoxaline structure, and a preparation method and an application thereof. The quinoxaline-containing triketone compound has a structure represented by general formula (I). The preparation method is mainly characterized in that a compound with a structure represented by formula (II) is contacted in the presence of an alkali and a solvent, and R1, R2, R3 and R4 in the formulas are respectively defined in the description. The quinoxaline-containing triketone compoundhas high herbicidal activity, and especially has an excellent effect of preventing and controlling broadleaf weeds and/or gramineous weeds, and the prevention and control effect is even better than that of some commercial herbicides sold in the market.
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Paragraph 0045-0047; 0052-0054; 0059-0061; 0066-0068
(2020/03/13)
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- Ruthenium(II) η6-arene complexes containing a dinucleating ligand based on 1,8-naphthyridine
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Ruthenium arene complexes, [(η6-p-cymene)2Ru2(L)Cl2](PF6)2 [3b, L = 2, 7-bis(di-2-pyridinyl)-1,8-naphthyridine] and [(η6-p-cymene)Ru(L′)Cl](PF6) [4, L′ = tri(2-pyridinyl)amine], were synthesized and characterized by spectroscopic and analytical techniques. The molecular structure of [(η6-p-cymene)2Ru2(L)Cl2]Cl2 (3a) was further determined by single-crystal X-ray analysis. The use of these ruthenium complexes as pre-catalysts for oxidative coupling of 1,2-diols/1,2-aminoalcohol with o-phenylenediamines leading to quinoxalines was investigated. Complex 3b appeared to be a good catalyst for this transformation.
- Tang, Wei-Hung,Liu, Yi-Hung,Peng, Shie-Ming,Liu, Shiuh-Tzung
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- Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation
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Gliomas are the most common and devastating tumors of the central nervous system (CNS). Many pieces of evidence point out the relevance of natural compounds for cancer therapy and prevention, including chalcones. In the present study, eight synthetic quin
- Mielcke, Tania R.,Mascarello, Alessandra,Filippi-Chiela, Eduardo,Zanin, Rafael F.,Lenz, Guido,Leal, Paulo César,Chirardia, Louise D.,Yunes, Rosendo A.,Nunes, Ricardo J.,Battastini, Ana M.O.,Morrone, Fernanda B.,Campos, Maria M.
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scheme or table
p. 255 - 264
(2012/03/26)
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- Novel Quinoxaline Derivatives and Their Medical Use
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This invention relates to novel quinoxaline derivatives having medical utility, to use of the quinoxaline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinoxaline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to positive modulation of AMPA receptor mediated synaptic responses.
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Page/Page column 6
(2009/12/05)
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- NOVEL ANTIMALARIA AGENT CONTAINING HETEROCYCLIC COMPOUND
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Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula -C(=O)-NH- or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
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Page/Page column 59
(2008/06/13)
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- NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
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Page/Page column 67
(2010/11/08)
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- SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
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The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes
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Page/Page column 40
(2008/06/13)
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- Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines
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A series of 29 new quinoxalines was synthesized and evaluated in vitro against several parasites (Leishmania donovani, Trypanosoma brucei brucei, and Trichomonas vaginalis). Several of them displayed interesting activities, and particularly four quinoxaline amides showed in vitro antileishmanial properties (IC50 less than 20 μM).
- Hui, Xu,Desrivot, Julie,Bories, Christian,Loiseau, Philippe M.,Franck, Xavier,Hocquemiller, Reynald,Figadere, Bruno
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p. 815 - 820
(2007/10/03)
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- A new family of quinoline and quinoxaline analogues of combretastatins
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The 3-hydroxy-4-methoxyphenyl ring of combretastatin A-4 can be replaced by a 2-naphthyl moiety without significant loss of cytotoxicity and inhibition of tubulin polymerization potency. In this paper we show that the 6- or 7-quinolyl systems can in turn replace both cyclic moieties, keeping in the first case most of the potency as cytotoxic agent and in the second case as inhibitor of tubulin polymerization, related to the activities displayed by model compounds.
- Perez-Melero, Concepcion,Maya, Ana B.S.,Del Rey, Benedicto,Pelaez, Rafael,Caballero, Esther,Medarde, Manuel
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p. 3771 - 3774
(2007/10/03)
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- Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
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Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
- Scapecchi, Serena,Martini, Elisabetta,Manetti, Dina,Ghelardini, Carla,Martelli, Cecilia,Dei, Silvia,Galeotti, Nicoletta,Guandalini, Luca,Romanelli, Maria Novella,Teodori, Elisabetta
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- Amide derivatives useful as inhibitors of the production of cytokines
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The invention concerns amide derivatives of formula (I) wherein R3is (1-6C)alkyl or halogeno; Q1is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2is a substituent such as hydroxy and halogeno; q is 0-4; and Q2includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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- Process for the preparation of 2,3-dihalogenoquinoxalines
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Quinoxalines are prepared by reaction of oxalic acid with an o-phenylenediamine, halogenation in the presence of a solvent and oxidation to a quinoxaline carboxylic acid derivative.
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