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Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, and surgery, as well as treating neurodegenerative diseases including Alzheimer’s disease, amyotrophic lateral sclerosis, Huntington’s disease, and Down’s syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, and inducing anesthesia are disclosed by administering to an animal in need of such treatment an alkyl or azido-substituted 1,4-dihydroquinoxaline-2, 3-dione or pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.

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Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. name: Quinoxaline-2,3(1H,4H)-dione, In a article, mentioned the application of 15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, molecular formula is C8H6N2O2

CuCN · 2,3-dihydroxyquinoxaline (1) can be crystallised by slowly cooling an acetonitrile solution of the components from 100 to 20C. 1 contains two polymeric isolated ?1[CuCN] chains within the open channels provided by hydrogen bonded stacks of 2,3-dihydroxyquinoxaline molecules. Positional disorder is observed for the C/N atoms of the bridging cyanide ligands within the effectively linear ?1[CuCN] chains, which exhibit angles of 169.9(2) at Cu and 171.8(6)/178.1(6) at the C/N atoms. Only very weak O . . . Cu interactions of 2.728(5) and 2.697(5) A are observed between the CuCN chains and the 2,3-dihydroxyquinoxaline stacks. Wiley-VCH Verlag GmbH, 2001.

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(Chemical Equation Presented) O-phenylene-diamine derivative containing colorimetric dinitroquinoxaline has been synthesized. Its UV-vis spectroscopy and 1H NMR investigation reveal that the receptor shows the strong binding ability for AcO-, F-, and H2PO 4-, moderate binding abilities for OH- and almost no binding abilities for Cl-, Br-, and I -. The interaction of the receptor with studied anions achieving the recognition of anions is proposed to come from the N – H. . .F and potential C – H. . .F hydrogen bonding in its neutral form. The results indicate that it is well suitable for the anion complexation, which is presumably contributed to its ring topology possessing a rigidity conjugation system. Moreover, the molecular orbital level of this receptor and its tautomer were further determined by means of theoretical investigations.

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Starting from 2,3-dichloroquinoxaline, a synthetic strategy for the preparation of 1-(3-phenylpropyl)-4-(pyridinylmethoxy)[1,2,4]triazolo[4,3-a]quinoxalines is described.

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Background We designed to synthesize a number of 2-(2-(substituted benzylidene) hydrazinyl)-N-(4-((3-(phenyl imino)-3,4-dihydro quinoxalin-2(1 H)-ylidene)amino) phenyl) acetamide S1-S13 with the hope to obtain more active and less toxic anti-microbial and anti-TB agents. Methods A series of novel quinoxaline Schiff bases S1-S13 were synthesized from o-phenylenediamine and oxalic acid by a multistep synthesis. In present work, we are introducing graph theoretical analysis to identify drug target. In the connection of graph theoretical analysis, we utilised KEGG database and Cytoscape software. All the title compounds were evaluated for their in-vitro anti-microbial activity by using agar well diffusion method at three different concentration levels (50, 100 and 150 mug/ml). The MIC of the compounds was also determined by agar streak dilution method. Results The identified study report through graph theoretical analysis were highlights that the key virulence factor for pathogenic mycobacteria is a eukaryotic-like serine/threonine protein kinase, termed PknG. All compounds were found to display significant activity against entire tested bacteria and fungi. In addition the synthesized scaffolds were screened for their in vitro antituberculosis (anti-TB) activity against Mycobacterium tuberculosis (Mtb) strain H 37 Ra using standard drug Rifampicin. Conclusion A number of analogs found markedly potent anti-microbial and anti-TB activity. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. The observed study report was showing that the compound S6 (4-nitro substitution) exhibited most potent effective anti-microbial and anti-TB activity out of various tested compounds.

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Until recently, discriminating between homomeric 5-HT3A and heteromeric 5-HT3AB receptors was only possible with ligands that bind in the receptor pore. This study describes the first series of ligands that can discriminate between these receptor types at the level of the orthosteric binding site. During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [3H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. Fragment hit exploration, initiated from VUF10166 and 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol, resulted in a series of compounds with higher affinity at either 5-HT3A or 5-HT3AB receptors. These ligands reveal that a single atom is sufficient to change the selectivity profile of a compound. At the extremes of the new compounds were 2-amino-3-(4-methylpiperazin-1-yl)quinoxaline, which showed 11-fold selectivity for the 5-HT3A receptor, and 2-(4-methylpiperazin-1-yl)quinoxaline, which showed an 8.3-fold selectivity for the 5-HT3AB receptor. These compounds represent novel molecular tools for studying 5-HT3 receptor subtypes and could help elucidate their physiological roles.

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Derivatives of the nonselective excitatory amino acid antagonist kynurenic acid (4-oxo-1,4-dihydroquinoline-2-carboxylic acid, 1) have been synthesized and evaluated for in vitro antagonist activity at the excitatory amino acid receptors sensitive to N-methyl-D-aspartic acid (NMDA), quisqualic acid (QUIS or AMPA), and kainic acid (KA).Introduction of substituents at the 5-, 7-, and 5,7-positions resulted in analogues having selective NMDA antagonist action, as a result of blockade of the glycine modulatory (or coagonist) site on the NMDA receptor.Regression analysis suggested a requirement for op timally sized, hydrophobic 5- and 7-substituents, with bulk tolerance being greater at the 5-position.Optimization led to the 5-iodo-7-chloro derivative (53), which is the most potent and selective glycine/NMDA antagonist to date (IC50 vs <3H>glycine binding, 32 nM; IC50’s for other excitatory amino acid receptor sites, >100 muM).Substitution of 1 at the 6-position resulted in compounds having selective non-NMDA antagonism and 8-substituted compounds were inactive at all receptors.The retention of glycine/NMDA antagonist activity in heterocyclic ring modified analogues, such as the oxanilide 69 and the 2-carboxybenzimidazole 70, suggests that the 4-oxo tautomer of 1 and its derivatives is required for activity.Structurally related quinoxaline-2,3-diones are also glycine/NMDA antagonists, but are not selective and are less potent than the 1 derivatives, and additionally show different structure-activity requirements for aromatic ring substitution.On the basis of these results, a model accounting for glycine receptor binding of the 1 derived antagonists is proposed, comprising (a) size-limited, hydrophobic binding of the benzene ring, (b) hydrogen- bond acceptance by the 4-oxo group, (c) hydrogen-bond donation by the 1-amino group, and (d) a Coulombic attraction of the 2-carboxylate.The model can also account for the binding of quinoxaline-2,3-diones, quinoxalic acids, and 2-carboxybenzimidazoles.

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Discover the magic of the Quinoxaline-2,3(1H,4H)-dione

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A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kalpha inhibitory activities. Among the synthesized target compounds, 17 (PI3Kalpha IC50: 0.07 muM) displayed the most potent cellular activities (IC50 values of 0.14 muM, 0.07 muM, 0.95 muM and 0.05 muM against PC3, A549, HCT116 and HL 60, respectively).

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Quinoxaline-2,3-(1H,4H)-diones of the formula I STR1 and their tautomeric and enantiomeric forms and their physiologically tolerated salts, the variables R, R 1 and R 2 have the meanings specified in claim 1, and are useful for therapeutic treatment of neurodegenerative disorders, neurotoxic disturbances or as antiepileptics, antidepressants and anxiolytics; and drugs composed thereof.

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Quality Control of Quinoxaline-2,3(1H,4H)-dione, New research progress on 15804-19-0 in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 15804-19-0, Name is Quinoxaline-2,3(1H,4H)-dione, molecular formula is C8H6N2O2. In a Article,once mentioned of 15804-19-0

Quinoxaline 1,4-dioxide (XIIIa) with acetic anhydride gave 1-acetoxy-2(1H)-quinoxalinone (XIVa) which was prone to facile hydrolysis to yield 1-hydroxy-2(1H)-quinoxalinone (XVa).Both XIVa and XVa were isolated from the reaction mixture.On prolonged heating with acetic anhydride, XIIIa, XIVa and XVa were converted slowly to the same end product, 2,3(1H,4H)-quinoxalinedione (XXa). 6-Ethoxy- (XIIIb), 6-methoxy- (XIIIc), and 6-methylquinoxaline 1,4-dioxide (XIIId) behaved similarly, except that the attack of the reagent took place exclusively on N-oxide para to the electron-donating substituents, and none of the other expected isomeric compounds XVIIb-d were isolated.Whereas 6-chloroqinoxaline 1,4-dioxide (XIIIe) bearing an electron-attracting chloro substituent on the benzene ring gave exclusively the other isomers XVIIe, XVIIIe, and XXe.A mechanism for this novel rearrangement is proposed and discussed.

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