Compounds for inhibiting drug-resistant strains of HIV-1 integrase
A technology of HIV-1 and compounds, applied in the field of compounds for inhibiting drug-resistant HIV-1 integrase drug-resistant strains
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[0174] Scheme B. Preparation of Starting Pyridine Analogs
[0175]
[0176] Scheme C. Preparation of 1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide analogs.
[0177]
[0178] Scheme D. 1-Hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide and 2-oxo-1,2-dihydro-1,8-naphthyridine- Preparation of 3-carboxamide analogues.
[0179]
[0180] Scheme E. Preparation of 1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide analogs.
[0181]
[0182] Scheme F. Preparation of 4-amino-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide analogs.
[0183]
[0184] The heck reaction: R 8 = alkenyl
[0185] Suzuki Reaction: R 8 = aryl
[0186] Sonogashira reaction: R 8 = Alkyl
[0187] Buchwald-Hartwig amination: R 8 = amine
[0188] Ullmann Response: R 8 = ether
[0189] Negishi reacts: R 8 = Alkyl
[0190] Scheme G. Preparation of 1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide analogs using coupling reactions.
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Embodiment
[0594] Assay protocol:
[0595] In vitro integrase assay. The integrase reaction was performed by adding drug or an equal volume of 100% dimethyl sulfoxide (DMSO; used as drug solvent) to 20 nM DNA and 400 nM integrase in 50 mM morpholine propane sulfonic acid (pH 7.2), 7.5 mM MgCl 2 and 14 mM 2-mercaptoethanol in a mixture. Reactions were performed at 37°C for 2 hours and quenched by adding an equal volume of loading buffer (formamide containing 1% sodium dodecyl sulfate, 0.25% bromophenol blue, and xylene cyanol). Reaction products were separated on a 16% polyacrylamide denaturing sequencing gel. Dried gels were visualized using a Typhoon 8600 (GE Healthcare, Piscataway, NJ). Densitometric analysis was performed using ImageQuant 5.1 software from GE Healthcare. Data analysis of at least 3 independent measurements was performed using GraphPad's Prism 5.0c software (linear regression, 50% inhibitory concentration [IC 50 ] determination, standard deviation [SD]).
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