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Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia

Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clinical trials in volunteers and primary insomnia patients. The relative contribution of antagonism of OX1R and OX2R for sleep induction is still a matter of debate. We therefore initiated a drug discovery project with the aim of creating both OX2R selective antagonists and DORAs. Here we report that the OX 2R selective antagonist 26 induced sleep in mice primarily by increasing NREM sleep, whereas the DORA suvorexant induced sleep largely by increasing REM sleep. Thus, OX2R selective antagonists may also be beneficial for the treatment of insomnia.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N528 | ChemSpider

Some scientific research about 6639-87-8

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 6639-87-8 is helpful to your research. Reference of 6639-87-8

Reference of 6639-87-8, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 6639-87-8, molcular formula is C8H5N3O2, introducing its new discovery.

Pressure Effects on the Thermal Decomposition of Nitramines, Nitrosamines, and Nitrate Esters

Solutions of nitramine and nitrate ester explosives and model compounds were thermolyzed at various hydrostatic pressures and their rates of decomposition were measured.The effects of pressure on their rates were used to infer the mechanism of their initial decomposition steps.Most nitramines, including the explosive octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine (HMX), appear to undergo homolysis of the N-NO2 bond, because their reaction rates decrease with increasing pressure.Exceptions are hexahydro-1,3,5-trinitro-1,3,5-triazine (RDX) and the model compound, 6-nitro-1,2-dinitroso-1,2,3,4-tetrahydroquinoxaline, which react faster with increasing pressure.These two compounds can aromatize by elimination of HNO2 and HNO, respectively.Secondary nitrate esters shift their major decomposition pathway from homolysis of the O-NO2 bond to elimination of HNO3 in the pressure range of 0.4 to 0.8 GPa.The elimination reaction resembles carboxylate ester pyrolysis with E1 character.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N964 | ChemSpider

Awesome and Easy Science Experiments about Quinoxalin-6-amine

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Synthetic Route of 6298-37-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.6298-37-9, Name is Quinoxalin-6-amine, molecular formula is C8H7N3. In a Article£¬once mentioned of 6298-37-9

Solvent-free synthesis of quinolone derivatives

Quinolones can be prepared in a three step procedure from triethylorthoformate and activated methylene derivatives leading to alkoxymethylenemalonates followed by reaction with aromatic amines and finally a cyclization. All the reactions were carried out under solvent-free conditions possibly under microwave activation with benefits for the first step.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N75 | ChemSpider

More research is needed about 25594-62-1

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25594-62-1, Name is 2-Acetylquinoxaline, belongs to quinoxaline compound, is a common compound. Safety of 2-AcetylquinoxalineIn an article, once mentioned the new application about 25594-62-1.

Mild and general method for the alpha-Arylation of heteroaromatic ketones

Chemical equation Presented The development of a general and mild method for Pd-catalyzed alpha-arylatlon of a variety of ketones bearing multiple heteroatoms Is described. The ligand to metal ratio and the position of the heteroatoms with respect to the carbonyl moiety significantly impact the efficiency of these transformations. In addition, these conditions were successfully applied to the alpha-arylation of cyclic imines. A detailed Investigation of the scope of this methodology, including the effect of the ligand to metal ratio, Is discussed.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N749 | ChemSpider

New explortion of 2213-63-0

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Synthetic Route of 2213-63-0, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.2213-63-0, Name is 2,3-Dichloroquinoxaline, molecular formula is C8H4Cl2N2. In a article£¬once mentioned of 2213-63-0

Conformational behavior of pyrazine-bridged and mixed-bridged cavitands: A general model for solvent effects on thermal “vase-kite” switching

The controllable switching of suitably bridged resorcin[4]arene cavitands between a “vase” conformation, with a cavity capable of guest inclusion, and a “kite” conformation, featuring an extended flattened surface, provides the basis for ongoing developments of dynamic molecular receptors, sensors, and molecular machines. This paper describes the synthesis, X-ray crystallographic characterization, and NMR analysis of the “vase-kite” switching behavior of a fully pyrazine-bridged cavitand and five other mixed-bridged quinoxaline-bridged cavitands with one methylene, phosphonate, or phosphate bridge. The pyrazine-bridged resorcin[4]arene cavitand displayed an unexpectedly high preference for the kite conformation in nonpolar solvents, relative to the quinoxaline-bridged analogue. This observation led to extensive solvent-dependent switching studies that provide a detailed picture of how solvent affects the thermal vase-kite equilibration. As for any thermodynamic process in the liquid phase, the conformational equilibrium is affected by how the solvent stabilizes the two individual states. Suitably sized solvents (benzene and derivatives) solvate the cavity of the vase form and reduce the propensity for the vase-to-kite transition. Correspondingly, the kite geometry becomes preferred in bulky solvents such as mesitylene, incapable of penetrating the vase cavity. As proposed earlier by Cram, the kite form is preferred at low temperatures due to the more favorable enthalpy of solvation of the enlarged surface. Furthermore, the kite conformation is more preferred in solvents with substantial hydrogen-bonding acidity: weak hydrogenbonding interactions between the mildly basic quinoxaline and pyrazine nitrogen atoms and solvent molecules are more efficient in the open kite than in the closed vase form. Vase-to-kite conversion is entirely absent in dipolar aprotic solvents lacking any H-bonding acidity. Thermal vase-kite switching requires fully quinoxaline- or pyrazinebridged cavitands, whereas pH-controlled switching is also applicable to systems incorporating only two or three such bridges.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N1523 | ChemSpider

Simple exploration of 3,4-Dihydroquinoxalin-2(1H)-one

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Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design

Bromodomains are key transcriptional regulators that are thought to be druggable epigenetic targets for cancer, inflammation, diabetes and cardiovascular therapeutics. Of particular importance is the first of two bromodomains in bromodomain containing 4 protein (BRD4(1)). Protein-ligand docking in BRD4(1) was used to purchase a small, focused screening set of compounds possessing a large variety of core structures. Within this set, a small number of weak hits each contained a dihydroquinoxalinone ring system. We purchased other analogs with this ring system and further validated the new hit series and obtained improvement in binding inhibition. Limited exploration by new analog synthesis showed that the binding inhibition in a FRET assay could be improved to the low muM level making this new core a potential hit-to-lead series. Additionally, the predicted geometries of the initial hit and an improved analog were confirmed by X-ray co-crystallography with BRD4(1).

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N159 | ChemSpider

Archives for Chemistry Experiments of 1448-87-9

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CERTAIN IMIDAZOQUINOXALINONES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS

This invention encompasses compounds of the formula: STR1 and the pharmaceutically acceptable non-toxic salts thereof wherein R 1, R. sub.2, R 3, R 4 are variables;

X and Y represent hydrogen, halogen, hydroxy or amino substituents, with the proviso that when Y is a hydrogen, halogen, or amino substituent, X is hydroxy; and< P>

W represent aryl groups unsubstituted or substituted with halogen, hydroxy, alkyl, alkoxy or amino groups.

These compounds or prodrugs thereof are highly selective agonists, antagonists or inverse agonists or GaBAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorder, overdose with benzodiazepine drugs, and enchancement of memory.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N487 | ChemSpider

Archives for Chemistry Experiments of 2-Chloroquinoxaline

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1448-87-9, Name is 2-Chloroquinoxaline, belongs to quinoxaline compound, is a common compound. name: 2-ChloroquinoxalineIn an article, once mentioned the new application about 1448-87-9.

Heterocyclic ether type phenoxy fatty acid derivatives and herbicidal composition

A herbicidal composition which comprises an adjuvant and an active ingredient of heterocyclic ether type phenoxy fatty acid derivative having the formula STR1 wherein A represents –CH– or –N–; X represents a halogen atom; n is 0, 1 or 2; R1 represents a hydrogen atom; a lower alkyl group; R2 represents –OH; –O-alkyl group; –OM group (M is an inorganic or organic salt moiety); STR2 –O-lower alkenyl group; –O-benzyl group; –O-lower alkylalkoxy group; –O-phenyl; –O-cyclohexyl, –O-halogenoalkyl, –O-lower alkynyl and –O-cyanoalkyl; R3 and R4 respectively represent a hydrogen atom or a lower alkyl group.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N489 | ChemSpider

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1448-87-9, Name is 2-Chloroquinoxaline, belongs to quinoxaline compound, is a common compound. Quality Control of 2-ChloroquinoxalineIn an article, once mentioned the new application about 1448-87-9.

Acetonitrile Derivatives as Carbonyl Synthons. One-Pot Preparation of Diheteroaryl Ketones via a Strategy of Sequential SNAr Substitution and Oxidation

The anion of 2-aryl acetonitrile derivatives reacted with a variety of heteroaryl chlorides or bromides in an SNAr manifold to afford intermediate anions which were susceptible to oxidation. The addition of sodium peroxide and aqueous NH4OAc solution effected oxidation to afford aryl heteroaryl ketones in good yields. Aryl acetonitrile derivatives are thus umpolung-type synthons of the corresponding aryl carbonyl functionality.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N729 | ChemSpider

More research is needed about 6-Methylquinoxaline

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 6344-72-5. In my other articles, you can also check out more blogs about 6344-72-5

Synthetic Route of 6344-72-5, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 6344-72-5, 6-Methylquinoxaline, introducing its new discovery.

The remarkable effect of a simple ion: Iodide-promoted transfer hydrogenation of heteroaromatics

I can do it! Accelerated by simple iodide ions, rhodium-catalysed transfer hydrogenation can be readily performed on quinolines, isoquinolines and quinoxalines, affording the tetrahydro products in high yields with low catalyst loading (see scheme). Copyright

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N43 | ChemSpider