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Reaction of phthalic acid with 2-methyl-4-N-phenylaminoquinoline under PPA condition resulted in the formation of 6-methyldibenzo[b, h][1,6]naphthyridines, whereas the same reaction with 2,4-bis(N-phenylamino)quinoline resulted in the dimeric dibenzo[b, h][1,6]naphthyridines. A novel mechanism has been proposed to explain the formation of the unexpected product. Screening for the antibacterial activity against various pathogens, proved that the dimeric analogs showed a better antibacterial activity when compared to their monomeric analogs.

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A highly site-selective amidation reaction of substituted 2,4-dichloroazines is reported. Palladium acetate/1,1?-bis(diphenylphosphino)ferrocene (dppf) was identified as the optimal catalyst system, producing >99:1 C-2/C-4 selectivity for most examples. The generality of this transformation was demonstrated through a survey of a diverse amide/substituted 2,4-dichloroazine scope, leading to the preparation of the desired C-2 amidated products in good to excellent yields.

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The present invention relates to 4-thio substituted quinoline and naphthyridine derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 4-thio substituted quinoline or naphthyridine derivative.

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The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators

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Compounds that inhibit at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.

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Analogues of 2-methoxypyridine undergo rearrangement to N-methylpyridones under flash vacuum pyrolysis (FVP) conditions. Ethoxy derivatives undergo competitive ethyl migration and elimination of ethylene. Analogues of 4-methoxypyridine do not undergo rearrangement under FVP conditions, but demethylation on silica may occur. The ease of rearrangement follows the basicity of the alkoxyhetarene to some extent. The vapour-phase rearrangements have been contrasted to condensed-phase pyrolyses. and a four-centre transition state for the former is supported by computation. The rearrangement allows structural assignment to the two products from the reaction of 2,4-dichloroquinoline with pyrrolidine.

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An alternative process of Pd-catalyzed C-4 selective coupling of 2,4-dichloropyridines with boronic esters was developed, which afforded 24 examples of C-4 coupled pyridines in moderate to good yields. After further arylation, 21 examples of C-2, C-4 diarylated pyridines with a significant photophysical property were obtained, which were applied as pyridine-based dyes into live-cell imaging with good biocompatibility and low toxicity.

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The invention discloses a quinoline substituted indole compound, containing the quinoline substituted indole compound of the pharmaceutical composition and its preparation method, also discloses quinoline substituted indole compound, containing the quinoline substituted indole compound of a pharmaceutical composition for pharmaceutical use, in particular in the preparation of medicament for treating tumor application, and preparation by inhibiting microtubule protein activity to treat other diseases or disorders of the application of the medicament. (by machine translation)

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Room temperature biacetyl phosphorescence enhanced via molecular organization is observed for many aromatic compounds.Micelles composed of sodium dodecyl sulfate(SDS) and hosts such as beta-cyclodextrin(beta-CD) are used to enhance the energy transfer reaction by organizing the reactants in close proximity to one another.The triplet-triplet energy transfer of several polynuclear aromatics, nitrogen heterocyclics, and heavy-atom-substituted species to biacetyl was evaluated.Both SDS and beta-CD were found to provide a superior medium for production of sensitized biacetylphosphorescence than found with homogenous solution.Typically,limits of detection of 1x 10-8 to 10-9 M in SDS and 1 x 10-7 M in beta-CD were obtained.The sensitivities of the methods are dependent on the solubility of the donor in SDS, the ability of the donor to fit into the beta-cyclodextrin cavity, and the background signal produced by the biacetyl blank solution.

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2,4-Disubstituted quinolines with additional substituents in positions 5-8 have been found to have anthelmintic properties. A number of 2,4-dimethoxy-6- or 8-arylquinolines have potent activity against the sheep nematode Haemonchus contortus, with LD99 values of the same order of magnitude as levamisole. These arylquinolines maintain their activity against levamisole-, ivermectin- and thiabendazole-resistant strains of H. contortus.

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