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15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, belongs to quinoxaline compound, is a common compound. Recommanded Product: Quinoxaline-2,3(1H,4H)-dioneIn an article, once mentioned the new application about 15804-19-0.

Novel compound, (E)-3-([1,2,4]triazolo[4,3-a]quinoxalin-4(5H)-on-1-yl)acrylic acid, containing triazole and quinoxaline moieties has been synthesized and characterized. The solubility of the compound in water and surfactant solutions has been estimated at different pH. It has been shown that the increase in solubility is due to hydrophobic effect as well as electrostatic interactions. The capability of this compound to integrate within dipalmitoylphosphocholine lipid bilayer has been evaluated. An increase in membranotropic properties after encapsulation of this compound in nanocontainers based on dicationic surfactant has been exhibited.

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To develop novel anti-inflammatory agents, a series of 5-alkyl-4-oxo-4,5-dihydro-[1, 2, 4]triazolo[4,3-a]quinoxaline-1-carboxamide derivatives were designed, synthesised, and evaluated for anti-inflammatory effects using RAW264.7 cells. Structures of the synthesised compounds were determined using 1H NMR, 13C NMR, and HRMS. All the compounds were screened for anti-inflammatory activity based on their inhibitory effects against LPS-induced NO release. Among them, 5-(3,4,5-trimethoxybenzyl)-4-oxo-4,5-dihydro-[1, 2, 4]triazolo[4,3-a]quinoxaline-1-carboxamide (6p) showed the highest anti-inflammatory activity and inhibited NO release more potently than the lead compound D1. Further studies revealed that compound 6p reduced the levels of NO, TNF-alpha, and IL-6, and that its anti-inflammatory activity involves the inhibition of COX-2 and iNOS and downregulation of the mitogen-activated protein kinases (MAPK) signal pathway. Notably, compound 6p displayed more prominent anti-inflammatory activity than D1 and the positive control ibuprofen in the in vivo acute inflammatory model. Overall, these findings indicate that compound 6p is a therapeutic candidate for the treatment of inflammation.

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Some new quinoxaline-6-sulfonamide and phthalazine-6-sulfonamide derivatives were synthesized. The majority of the prepared compounds showed antibacterial activity.

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Electric Literature of 15804-19-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, molecular formula is C8H6N2O2. In a Article,once mentioned of 15804-19-0

Homology modeling was used to build 3D models of the N-methyl-D-aspartate (NMDA) receptor glycine binding site on the basis of an X-ray structure of the water-soluble AMPA-sensitive receptor. The docking of agonists and antagonists to these models was used to reveal binding modes of ligands and to explain known structure-activity relationships. Two types of quantitative models, 3D-QSAR/CoMFA and a regression model based on docking energies, were built for antagonists (derivatives of 4-hydroxy-2-quinolone, quinoxaline-2,3-dione, and related compounds). The CoMFA steric and electrostatic maps were superimposed on the homology-based model, and a close correspondence was marked. The derived computational models have permitted the evaluation of the structural features crucial for high glycine binding site affinity and are important for the design of new ligands.

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Compounds and compositions are disclosed, which are useful as inhibitors of acetyltransferase Eis, a mediator of kanamycin resistance in Mycobacterium tuberculosis.

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15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, belongs to quinoxaline compound, is a common compound. Quality Control of Quinoxaline-2,3(1H,4H)-dioneIn an article, once mentioned the new application about 15804-19-0.

A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure- activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H- imidazol-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a K(i) value of 0.084 muM, being approximately equipotent with 2,3-dihydro-6-nitro- 7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; K(i) = 0.060 muM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).

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Abstract: Many shreds of evidence have recently correlated A2B receptor antagonism with anticancer activity. Hence, the search for an efficient A2B antagonist may help in the development of a new chemotherapeutic agent. In this article, 23 new derivatives of [1,2,4]triazolo[4,3-a]quinoxaline were designed and synthesized and its structures were confirmed by different spectral data and elemental analyses. The results of cytotoxic evaluation of these compounds showed six promising active derivatives with IC50 values ranging from 1.9 to 6.4 muM on MDA-MB 231 cell line. Additionally, molecular docking for all synthesized compounds was performed to predict their binding affinity toward the homology model of A2B receptor as a proposed mode of their cytotoxic activity. Results of molecular docking were strongly correlated with those of the cytotoxic study. Finally, structure activity relationship analyses of the new compounds were explored. Graphic abstract: [Figure not available: see fulltext.].

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Reference of 15804-19-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, molecular formula is C8H6N2O2. In a Article,once mentioned of 15804-19-0

Transition metal complexes of thiosemicarbazones with quinoxaline hub: An emphasis on antidiabetic property

New transition metal complexes of quinoxaline-thiosemicarbazone ligands were prepared and characterised by spectroanalytical techniques. The ligands L1H2 and L2H2 were obtained by the reaction of quinoxaline-2.3(1,4H)-dione with methyl and phenyl thiosemicarbazide, respectively. All the complexes are found to be monomeric in nature and have tetrahedral geometry. The copper complexes have shown redox responses in the applied voltage range, whereas the ligands and other complexes are electrochemically innocent. The ligands, copper and zinc complexes are explored for antidiabetic activity in the diabetes-induced Wister rats. Evaluation of antidiabetic activity was done by blood-glucose test and oral glucose tolerance test; few compounds have exhibited significant antidiabetic activity and posses low toxicity with a high safety profile. Springer Science+Business Media, LLC 2011.

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A NEW METHOD FOR SYNTHESIS OF LACTAM

2-Substituted 3-oxo-3,4-dihydroquinoxalines were oxidized with H2O2 to 2,3-dioxo-1,2,3,4-tetrahydroquinoxaline.This oxidation of the imino bonding in the heterocycles to the lactam was assumed to proceed via the various peroxides, but not via the oxaziranes.

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Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)- ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors

A series of 4-hydroxy-3-nitroquinolin-2(1H)-ones (HNQs) was synthesized by nitration of the corresponding 2,4-quinolinediols. The HNQs were evaluated as antagonists at the glycine site of NMDA receptors by inhibition of [3H]DCKA binding to rat brain membranes. Selected HNQs were also tested for functional antagonism by electrophysiological assays in Xenopus oocytes expressing either 1a/2C subunits of NMDA receptors or rat brain AMPA receptors. The structure-activity relationships (SAR) of HNQs showed that substitutions in the 5-, 6-, and 7-positions in general increase potency while substitutions in the 8-position cause a sharp reduction in potency. Among the HNQs tested, 5,6,7-trichloro HNQ (8i) was the most potent antagonist with an IC50 of 220 nM in [3H]DCKA binding assay and a K(b) of 79 nM from electrophysiological assays. Measured under steady-state conditions HNQ 8i is 240-fold selective for NMDA over AMPA receptors. The SAR of HNQs was compared with those of 1,4-dihydroquinoxaline-2,3-diones (QXs) and 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes (QTOs). In general, HNQs have similar potencies to QXs with the same benzene ring substitution pattern but are about 10 times less active than the corresponding QTOs. HNQs are more selective for NMDA receptors than the corresponding QXs and QTOs. The similarity of the SAR of HNQs, QXs, and QTOs suggested that these three classes of antagonists might bind to the glycine site in a similar manner. With appropriate substitutions, HNQs represent a new class of potent and highly selective NMDA receptor glycine site antagonists.

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