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4-THIO SUBSTITUTED QUINOLINE AND NAPHTHYRIDINE COMPOUNDS

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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Synthesis of new 2-, 3-, and 4-substituted azidoquinolines: Inhibitors of human blood platelet aggregation in vitro

A series of 2-, 3- and 4-substituted azidoquinoline derivatives were synthesized and tested for their ability to inhibit human platelet aggregation in vitro triggered by adenosine diphosphate (15 muM), collagen (5 mug/ml), platelet activating factor (10 muM), or the stable prostaglandin H2 mimetic, U46619 (4 muM). The most active compounds (IC50 2.5-68.3 muM) were the geminal 3,3-diazides (4f and 4g) and the 4-azido-3-nitroquinolines (6f and 6g).

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Studies of the reactions between indole-2,3-diones (isatins) and 2-aminobenzylamine

Reflux of equimolecular amounts 2-aminobenzylamine and isatins in acetic acid produced indolo[3,2-c]quinolin-6-ones in good yields. A proposed mechanism involving initial formation of a spiro compound is given. This isolable intermediate subsequently rearranges via a sequential isocyanate ring opening and a cyclisation process to a urea derivative which finally cyclized to the indolo[3,2-c]quinolin-6-ones. The urea derivative could be prepared separately and cyclized selectively to indolo[3,2-c]quinolin-6-one. Reaction of N-acetylisatin with 2-aminobenzylamine at room temperature yielded the 1,4-benzodiazepinone 3-(2-acetamidophenyl)-1,5-dihydro-1,4-benzodiazepin-2-one whereas its isomer 2(2-acetamidophenyl)-4,5-dihydro-1,4-benzodiazepin-3-one was obtained from 2-(2-acetylaminophenyl)-N-(2-aminobenzyl)-2-oxoacetamide in acetic acid at room temperature. The previously unknown linear isomer of indolo[3,2-c]quinolin-6-one, i.e. indolo[2,3-b]quinolin-11-one, has been prepared by thermal (260C) cyclization of methyl 2-phenylamino indole-3-carboxylate, which in turn was prepared in two steps from methyl indole-3-carboxylate.

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Synthetic Approaches to 5,7- and 5,8-Dimethoxyquinoline. Sonochemical Dehalogenation of Substituted 2,4-Dichloroquinolines. Use of the 2D COLOC Spectrum for the NMR Assignment of 5,8-Dimethoxyquinoline

Sonochemical dehalogenation of 2,4-dichloroquinoline is very facile.However, with 5,7-dimethoxy-2,4-dichloroquinoline the reaction proceeds stepwise to provide the title dimethoxyquinolines which cannot be prepared via the Skraup reaction.The 13C NMR chemical shift assignments for 5,8-dimethoxyquinoline are presented.These were made by utilising the coupling connectivities from the bridgehead carbons in the 2D COLOC spectrum. – Keywords.Sonochemistry; Quinolines; 13C NMR Spectroscopy; 2D COLOC spectrum.

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HETEROCYCLIC DERIVATIVES AND USE THEREOF

The present invention relates to novel heterocyclic compounds useful in preparing drugs for the prevention or treatment of diseases associated with STAT3 protein. Specifically, these drugs are useful in the prevention or treatment of solid tumors, blood cancers, radiation or drug-resistant cancers, metastatic cancers, inflammatory diseases, immune system diseases, diabetes, macular degeneration, papillomavirus infections and tuberculosis.

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Synthesis of 2-alkynylquinolines from 2-chloro and 2,4-dichloroquinoline via Pd/C-catalyzed coupling reaction in water

The Pd/C-CuI-PPh3 catalyst system facilitated Sonogashira coupling of 2-chloroquinoline and 2,4-dichloroquinoline with terminal alkynes in water without generating any significant side products. A variety of 2-alkynylquinolines were prepared from 2-chloroquinoline in good to excellent yields and the 2,4-dichloroquinoline afforded monosubstituted product i.e., 2-alkynyl-4-chloro quinoline with high regioselectivity. The methodology was found to be effective for the alkynylation of 1-chloroisoquinoline and 3-methyl-2-chloroquinoline.

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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 1055361-35-7 is helpful to your research. COA of Formula: C19H11F3N2O4S

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Chemistry of 4-Hydroxy-2(1H)-quinolone. Part 1: Synthesis and reactions

This review summarizes results from the literature concerning the synthesis and chemical reactivity of 4-hydroxy-2(1H)-quinolone as well as its reactions that are reported. Most imaginable reaction types have been successfully applied and used, as many of the synthetized compounds exhibit interesting biological activity in various fields.

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ARYL-SUBSTITUTED IMIDAZOLES AND METHODS OF MAKING AND USING SAME

The compounds of the invention are antagonists of MDM2 and/or MDMX, with excellent specificity for MDM2 and/or MDMX over other proteins. Several analogs demonstrate selective binding affinity to MDMX over MDM2. The disclosed compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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Chemistry can be defined as the study of matter and the changes it undergoes. HPLC of Formula: C19H11F3N2O4S. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.HPLC of Formula: C19H11F3N2O4S, Name is 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, molecular formula is C19H11F3N2O4S, introducing its new discovery.

Regioselective alkynylation followed by Suzuki coupling of 2,4-dichloroquinoline: Synthesis of 2-alkynyl-4-arylquinolines

A two step synthesis of 2-alkynyl-4-arylquinolines has been accomplished via Pd/C-mediated regioselective C-2 alkynylation of 2,4-dichloroquinoline in water followed by Suzuki coupling at C-4 of the resulting 4-chloro derivative.

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Molecular Docking Studies and Synthesis of Amino-oxy-diarylquinoline Derivatives as Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors

In this study, amino-oxy-diarylquinolines were designed using structure-guided molecular hybridization strategy and fusing of the pharmacophore templates of nevirapine (NVP), efavirenz (EFV), etravirine (ETV, TMC125) and rilpivirine (RPV, TMC278). The anti-HIV-1 reverse transcriptase (RT) activity was evaluated using standard ELISA method, and the cytotoxic activity was performed using MTT and XTT assays. The primary bioassay results indicated that 2-amino-4-oxy-diarylquinolines possess moderate inhibitory properties against HIV-1 RT. Molecular docking results showed that 2-amino-4-oxy-diarylquinolines 8(a-d) interacted with the Lys101 and His235 residue though hydrogen bonding and interacted with Tyr318 residue though pi-pi stacking in HIV-1 RT. Furthermore, 8a and 8d were the most potent anti-HIV agents among the designed and synthesized compounds, and their inhibition rates were 34.0% and 39.7% at 1 muM concentration. Interestingly, 8a was highly cytotoxicity against MOLT-3 (acute lymphoblastic leukemia), with an IC 50 of 4.63¡À0.62 mug/mL, which was similar with that in EFV and TMC278 (IC 50 7.76¡À0.37 and 1.57¡À0.20 mug/ml, respectively). Therefore, these analogs of the synthesized compounds can serve as excellent bases for the development of new anti-HIV-1 agents in the near future.

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