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Preparation of derivatives of 1-(2-pyrimidinyl)piperazine as potential antianxiety, antidepressant, and antipsychotic agents

(Chemical Equation Presented) This paper describes the preparation of twenty-eight derivatives of 1-(2-pyrimidinyl)piperazine as potential antianxiety, antidepressant, and antipsychotic agents. In twenty-six of the preparations a chloro nitrogen heterocycle was caused to react with an excess of 1-(2-pyrimidinyl)piperazine in the absence of solvent. A specific example is given above.

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Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

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The important role of 2-Chloro-3-methylquinoxaline

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Pyrazolo[4?,3?:5,6]pyrano[2,3-b]quinoxalin-4(1H)-one: Synthesis and characterization of a novel tetracyclic ring system

(Chemical Equation Presented) Derivatives of the hitherto unknown ring system, pyrazolo[4?,3?:5,6]pyrano[2,3-b]quinoxalin-4(1H)-one, are synthesized in one step from the corresponding 1-substuituted or 1,3-disubstituted 2-pyrazolin-5-ones and 3-chloroquinoxaline-2-carbonyl chloride using calcium hydroxide in boiling 1,4-dioxane. The parent system carrying no substituent in positions 1 and 3 is obtained upon treatment of the 1-PMB (p-methoxybenzyl) protected congener with trifluoroacetic acid. Detailed NMR spectroscopic investigations including unambiguous chemical shift assignments of all 1H, 13C, and 15N resonances of the obtained tetracycles are reported.

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THE SYNTHESES OF NOVEL 2-(2-QUINOXALINYL)PYRIDAZIN-3(2H)-ONES

The first syntheses of 4-chloro-2-(2-quinoxalinyl)-pyridazin-3(2H)-one derivatives are reported.They could be synthesized from 2-hydrazinoquinoxaline derivatives as starting materials.

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FeCl3 catalysed 7-membered ring formation in a single pot: A new route to indole-fused oxepines/azepines and their cytotoxic activity

Various oxepine and azepine fused N-heterocyclic derivatives were synthesized using a new and one-pot reaction of 2,3-dichloro quinoxaline/pyrazine with 2-(1H-indol-2-yl)phenol/aniline in the presence of 25 mol% FeCl3. The reaction proceeded via C-C bond followed by C-X (X = O or N) bond formation to construct the central 7-membered ring, affording the desired products in good yields. The structure assignment was confirmed by the single crystal X-ray analysis of a synthesized oxepine fused N-heterocycle derivative. Most of the synthesized compounds were found to be promising when tested for their anti-proliferative properties against cervical and breast cancer cell lines.

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New explortion of Quinoxaline-5-carboxylic acid

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AMIDO-SUBSTITUTED AZASPIRO DERIVATIVES AS TANKYRASE INHIBITORS

The present invention relates to amido-substituted cyclohexane compounds of general formula (I) : in which A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.

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Present status of quinoxaline motifs: Excellent pathfinders in therapeutic medicine

Quinoxalines belong to a class of excellent heterocyclic scaffolds owing to their wide biological properties and diverse therapeutic applications in medicinal research. They are complementary in shapes and charges to numerous biomolecules they interact with, thereby resulting in increased binding affinity. The pharmacokinetic properties of drugs bearing quinoxaline cores have shown them to be relatively easy to administer either as intramuscular solutions, oral capsules or rectal suppositories. This work deals with recent advances in the synthesis and pharmacological diversities of quinoxaline motifs which might pave ways for novel drugs development.

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Archives for Chemistry Experiments of 2,3-Dichloroquinoxaline

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ANTIMICROBIAL AGENTS

The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.

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Static and Dynamic Properties of Quinoxalines in the Phosphorescent Triplet State from Optically Detected Magnetic Resonance

The static and dynamic properties of the phosphorescent triplet states of quinoxaline and 2,3-disubstituted derivatives in hexane have been studied at 1.4 K using the methods of optically detected magnetic resonance.In addition, the absorption and phosphorescence excitation spectra have also been measured to attain the information about the low lying excited states.A systematic comparison has been made for the purpose of examining the effect of substitution.A significant enhancement of the pumping rates for the y spin sublevel observed in the chlorine-substituted derivatives is concluded to be due to the additional indirect process of intersystem crossing which occurs from S1 of n,?* to T1 passing through the intermediate triplet state of ?,?*.A detailed discussion on the observed phosphorescence spectra originating from the three sublevels has achieved a satisfactory success in understanding the mechanisms responsible for the radiative decay processes.It is concluded that the mechanisms due to vibronic coupling with closely lying n,?* triplet states are of little importance in the systems studied here.

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New explortion of Quinoxalin-6-ylmethanol

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Method for preparing heterocyclic-carboxylic acids

The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous suspension of a 5- or 6-hydroxymethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.

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