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The second-generation of highly potent hepatitis C virus (HCV) NS3/4A protease inhibitors: Evolutionary design based on tailor-made amino acids, synthesis and major features of bio-activity

Hepatitis C is a current pandemic liver disease caused by the hepatitis C virus (HCV) with high morbidity and mortality. Recently, the direct-acting antiviral agents (DAAs) targeting HCV NS3/4A, NS5A and NS5B have become the most effective therapies against HCV infection in the clinical treatment. Among them, the second-generation of NS3/4A inhibitors have emerged as the mainstay of the DAA therapies, which are derived from the peptide substrate of NS3/4A protease and modified with various tailor-made amino acids in order to achieve high sustained virologic response (SVR) against HCV. This review summarizes sixteen examples of the second-generation of HCV NS3/4A inhibitors, mainly focusing on the clinical application, structure development, structure-activity relationship (SAR) and their synthesis.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N715 | ChemSpider

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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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Synthesis, Properties, and Reactivity of Bis-BN Phenanthrenes: Stepwise Bromination of the Main Scaffold

Two bis-BN phenanthrenes have been synthesized. Their photophysical properties are different from those of the reported mono-BN phenanthrenes. Moreover, the stepwise bromination of bis-BN phenanthrene 8 gave a series of brominated bis-BN phenanthrenes, with all of the mono-, di-, tri-, and tetrabrominated bis-BN phenanthrenes being successfully isolated and characterized. In addition, preliminary results showed that mono- and dibrominated species can be further functionalized by cross-coupling reactions.

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Archives for Chemistry Experiments of Quinoxaline-2,3(1H,4H)-dione

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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 application about 2-Chloroquinoxaline

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HETEROCYCLIC LIPXON ANALOGS AND USES THEROF

The present invention relates to a compound of formula (I): wherein L is an optionally substituted heterocyclic group excluding unsubstituted monocyclic pyridine groups; wherein a is 0, 1 or 2; wherein R1 is H or with R2 is a bond; wherein R2 is an optionally substituted alkoxy or aryloxy group, or with R1 forms a bond; wherein R3 is an optionally substituted alkyl group; and wherein R4 is CH2, CMe2 or O. Such compounds may be used in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis.

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DNA topoisomerase II inhibition has the activity of modulating kui analogue and its preparation method and application (by machine translation)

The invention discloses a DNA topoisomerase II inhibition activity of modulating kui analogs, its optical isomers, non-enantiomer or a racemic mixture, or its pharmaceutically acceptable salt, solvate, or a prodrug thereof, intermediate or metabolites thereof, the structure of the general formula (I) as shown: Wherein R1 , R2 , R3 , R4 , R5 And Ar in every one of the as defined in this invention. The invention also discloses a process for their preparation, their use as medicament and their application in treating tumors. The compounds of this invention curative effect is precise, small toxic side effect, enriched with the topoisomerase II technology is used for the expression of the drug for the treatment of diseases caused by abnormal inhibitors of types, it is expected to become therapeutic index higher can be used for clinical medicine. (by machine translation)

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Simple exploration of 2213-63-0

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Synthesis of 1-(3-phenylpropyl)-4-(pyridinylmethoxy)-[1,2,4]triazolo[4,3-a] quinoxalines

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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Solvent-free reaction using phosphonium salts: Chlorination of hydroxyheteroaromatics and dehydration of primary amides

Solvent-free chlorination of heteroaromatics using the phosphonium salt, prepared by reaction of triphenylphosphine with N-chlorosuccinimide, was accomplished by microwave-irradiation or heating to give the corresponding chloroheteroaromatics. Similarly, primary amides was converted into nitriles by this method.{A figure is presented}.

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Tethering identifies fragment that yields potent inhibitors of human caspase-1

Disulfide Tethering was applied to the active site of human caspase-1, resulting in the discovery of a novel, tricyclic molecular fragment that selectively binds in S4. This fragment was developed into a class of potent inhibitors of human caspase-1. Several key analogues determined the optimal distance of the tricycle from the catalytic residues, the relative importance of various features of the tricycle, and the importance of the linker.

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Pyridinium N-heteroarylaminides: A brief study of the synthesis and reactivity under solvent-free mechanochemical conditions

The first example of a heterocyclic aromatic substitution by an N-ylide and the first examples of heteroaromatic halogenations in the presence of N-halosuccinimides using mechanochemical conditions are described. ARKAT USA, Inc.

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Quinoxaline – Wikipedia,
Quinoxaline | C8H6N557 | ChemSpider