Can You Really Do Chemisty Experiments About 6-Nitroquinoxaline

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HETEROCYCLIC DERIVATIVES THAT ARE USED IN THE TREATMENT OF NEURODEGENERATIVE DISEASES

The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr?X?CHR1R2 (I) in which: -HetAr represents a group chosen from: ?X represents a linear, saturated or unsaturated, hydrocarbon-based chain comprising from 8 to 22 carbon atoms, optionally interrupted by an ?NH? or ?NH?CO? group, ?R1 represents a hydrogen atom or an ?OH, ?O(C1-C6)alkyl, ?OCO((C1-C6)alkyl), ?OSO2((C1-C6)alkyl) or ?OSO3H group, and ?R2 represents a hydrogen atom or a (C2-C6)alkynyl, (C2-C6)alkenyl or (C3-C6)cycloalkyl group. The present invention also relates to a process for preparing the compounds of Formula (I), and also to the use thereof, especially in the treatment of neurodegenerative diseases.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N935 | ChemSpider

Extracurricular laboratory:new discovery of Quinoxaline-2,3(1H,4H)-dione

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Synthesis of some 4-substituted hydrazinotetrazolo[1,5-a]quinoxalines

Reaction of 2,3 diketoquinoxaline in presence of phosphorus pentachloride and sodium azide in methanol gives 4-hydroxy tetrazolo[1,5-a]quinoxaline 3 which on reaction with phosphorous oxychloride gives 4-chloro tetrazolo[1,5-a] quinoxaline 4. This on treatment with hydrazine hydrate in ethanol yields 4-hydrazino tetrazolo[1,5-a]quinoxaline 5, which on reaction with various aldehydes in DMF gives 4-substituted hydrazinotetrazolo [1,5-a]quinoxalines 6a-g. The structures of compounds 6a-g have been confirmed by IR and 1H NMR.

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Awesome and Easy Science Experiments about 6-Methylquinoxaline

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Studies on New Acidic Azoles as Glucose-Lowering Agents in Obese, Diabetic db/db Mice

Bioisosteric substitution was used as a tool to generate several new structural alternatives to the thiazolidine-2,4-dione and tetrazole heterocycles as potential antidiabetic agents.Among the initial leads that emerged from this strategy, a family of acidic azoles, isoxazol-3- and -5-ones and a pyrazol-3-one, showed significant plasma glucose-lowering activity (17-42percent reduction) in genetically obese, diabetic db/db mice at a dose of 100 mg/kg/day * 4.Structure-activity relationship studies determined that 5-alkyl-4-(arylmethyl)pyrazol-3-ones, which exist in solution as aromatic enol/iminol tautomers, were the most promising new class of potential antidiabetic agent (32-45percent reduction at 20 mg/kg/d *4).Included in this work are convenient syntheses for several types of acidic azoles that may find use as new acidic bioisosteres in medicinal chemistry such as the antidiabetic lead 5-(trifluoromethyl)pyrazol-3-one (hydroxy tautomer) and aza homologs of the pyrazolones, 1,2,3-triazol-5-ones (hydroxy tautomer) and 1,2,3,4-tetrazol-5-one heterocycles. log P and pKa data for 15 potential acidic bioisosteres, all appended to a 2-naphthalenylmethyl residue so as to maintain a similar distance between the acidic hydrogen and arene nucleus, are presented.This new data set allows comparison of a wide variety of potential acid mimetics (pKa 3.78-10.66; log P -0.21 to 2.76) for future drug design.

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Final Thoughts on Chemistry for 15804-19-0

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Quantitative cascade condensations between o-phenylenediamines and 1,2-dicarbonyl compounds without production of wastes

o-Phenylenediamines 1 underwent a series of cascade condensations with 1,2-dicarbonyl compounds to afford quantitative yields (eight cases) of heterocycles in solid-state syntheses that avoided waste formation. The products were produced in pure form and did not require purifying workup. The components were ball-milled in stoichiometric ratio, or in exceptional cases they were melted together and heated in the absence of solvents (some of them giving quantitative yields). Benzils and 2-hydroxy-1,4-naphthoquinone afforded quinoxaline derivatives 3 and 5, 2-oxoglutaric acid gave a 3-oxodihydroquinoxaline 7, and oxalic acid afforded the dihydroquinoxaline-2,3-dione 9. This last condensed with la in the melt, to afford a mixture of bis(benzimidazolyl) 10 and fluoflavin 11. Alloxane hydrate provided a 100% yield of the 3-oxodihydroquinoxaline-2-carbonylureas 15/16 at room temperature. Parabanic acid required a melt reaction providing a 78% yield of 3-oxodihydroquinoxalinyl-2-urea 22 and side products. Despite numerous reaction steps, most of these uncatalyzed stoichiometric reactions proceeded quantitatively in the solid state to give only one product (plus water), with unsurpassed atom economy. If catalysis with HCl was tried, the results were inferior. If melt reactions were required it appeared to be advantageous to have the products crystallize directly at the reaction temperature. The synthetic results have been interpreted mechanistically and compared to some similar solution reactions that do not exhibit the benefits of the solid-state techniques. Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002).

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Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme

Infection by human immunodeficiency virus still represents a continuous serious concern and a global threat to human health. Due to appearance of multi-resistant virus strains and the serious adverse side effects of the antiretroviral therapy administered, there is an urgent need for the development of new treatment agents, more active, less toxic and with increased tolerability to mutations. Quinoxaline derivatives are an emergent class of heterocyclic compounds with a wide spectrum of biological activities and therapeutic applications. These types of compounds have also shown high potency in the inhibition of HIV reverse transcriptase and HIV replication in cell culture. For these reasons we propose, in this work, the design, synthesis and biological evaluation of quinoxaline derivatives targeting HIV reverse transcriptase enzyme. For this, we first carried out a structure-based development of target-specific compound virtual chemical library of quinoxaline derivatives. The rational construction of the virtual chemical library was based on previously assigned pharmacophore features. This library was processed by a virtual screening protocol employing molecular docking and 3D-QSAR. Twenty-five quinoxaline compounds were selected for synthesis in the basis of their docking and 3D-QSAR scores and chemical synthetic simplicity. They were evaluated as inhibitors of the recombinant wild-type reverse transcriptase enzyme. Finally, the anti-HIV activity and cytotoxicity of the synthesized quinoxaline compounds with highest reverse transcriptase inhibitory capabilities was evaluated. This simple screening strategy led to the discovery of two selective and potent quinoxaline reverse transcriptase inhibitors with high selectivity index.

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Top Picks: new discover of 7-Bromo-1-methyl-1H-quinoxalin-2-one

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Copper-catalyzed C-H/N-H cross-coupling reactions for the synthesis of 3-heteroaryl quinoxalin-2(1: H)-ones

An effective copper-catalyzed direct C-H/N-H cross-coupling of quinoxalin-2(1H)-ones with diverse unprotected 2-quinoxalinones and 2-quinolinones has been developed. This protocol provides a convenient route, with broad substrate scope, good functional group tolerance, and high atom economy, to various important quinoxalin-2(1H)-one-containing biheteroaryls, which are privileged structures in many biologically active compounds.

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More research is needed about 1865-11-8

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Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives

A series of pyrazine and quinoxaline derivatives have been synthesized, and their activity against M. tuberculosis (Mtb) and Mycobacterium avium (MAC) are reported. The 4-acetoxy-benzyl ester of pyrazinoic acid and 4?-acetoxybenzyl 2-quinoxalinecarboxylate showed excellent activity against Mtb (MIC ranges of less than 1-6.25 mug/mL) but only modest activity against MAC (MICs of 4-32 mug/mL).

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The Absolute Best Science Experiment for 6344-72-5

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PROCESSES FOR PREPARING GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS

The present invention relates to methods of making Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists. ”

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Properties and Exciting Facts About Quinoxalin-6-amine

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(2-Imidazolin-2-ylamino) substituted -quinoxalines and -quinazolines as antihypertensive agents

Novel (2-imidazolin-2-ylamino) substituted quinoxalines and -quinazolines, their preparation and use as antihypertensive agents are described.

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Final Thoughts on Chemistry for 2,3-Dichloroquinoxaline

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Synthesis, characterization, and optical properties of new metal complexes with the multi-sulfur 1,2-dithiolene ligand

Metal complexes containing a new multi-sulfur atom containing 1,2-dithiolene ligand, [4?,5?:5,6] [1,4] dithiino[2,3-b] quinoxaline-1?,3?-dithiolate, have been synthesized and characterized by electrochemical measurements, IR, UV-NIR and ESR spectroscopies. X-ray structure analysis reveals that the anions of the Ni-complex derived from the new ligand form a zig-zag chain along the b axis, and the anions of Au complex of the ligand stack along the a axis while the cations occupy the holes. The Ni-complex exhibits remarkable absorption at 1082 nm (epsilon = 15 000 dm3 mol-1 cm-1) and good solubility that render this complex as a promising near-IR dye for Q-switching neodymium lasers. The third-order non-linear optical properties of the complexes are measured by the Z-scan technique with a 6.5 ns pulsed laser at 532 nm. The Au complexes exhibit non-linear optical absorptive abilities, while the non-linear absorption of the nickel complex is negligible. All of the complexes show effective self-defocusing performance. The third-order non-linear optical susceptibilities for the Au complexes have been determined to be of the order of 10-13 esu.

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