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Philippe Cotelle - One of the best experts on this subject based on the ideXlab platform.
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magnesium chelating 2 hydroxyisoquinoline 1 3 2h 4h Diones as inhibitors of hiv 1 integrase and or the hiv 1 reverse transcriptase ribonuclease h domain discovery of a novel selective inhibitor of the ribonuclease h function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Frauke Christ, Zeger Debyser, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this ...
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Magnesium chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-Diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Zeger Debyser, C. Christ, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this compound on three different viral strains. Experimental data suggest that the antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Dione is probably due to the RNase H inhibition.
Muriel Billamboz - One of the best experts on this subject based on the ideXlab platform.
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magnesium chelating 2 hydroxyisoquinoline 1 3 2h 4h Diones as inhibitors of hiv 1 integrase and or the hiv 1 reverse transcriptase ribonuclease h domain discovery of a novel selective inhibitor of the ribonuclease h function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Frauke Christ, Zeger Debyser, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this ...
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Magnesium chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-Diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Zeger Debyser, C. Christ, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this compound on three different viral strains. Experimental data suggest that the antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Dione is probably due to the RNase H inhibition.
Herve Vezin - One of the best experts on this subject based on the ideXlab platform.
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magnesium chelating 2 hydroxyisoquinoline 1 3 2h 4h Diones as inhibitors of hiv 1 integrase and or the hiv 1 reverse transcriptase ribonuclease h domain discovery of a novel selective inhibitor of the ribonuclease h function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Frauke Christ, Zeger Debyser, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this ...
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Magnesium chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-Diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Zeger Debyser, C. Christ, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this compound on three different viral strains. Experimental data suggest that the antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Dione is probably due to the RNase H inhibition.
Nadia Touati - One of the best experts on this subject based on the ideXlab platform.
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magnesium chelating 2 hydroxyisoquinoline 1 3 2h 4h Diones as inhibitors of hiv 1 integrase and or the hiv 1 reverse transcriptase ribonuclease h domain discovery of a novel selective inhibitor of the ribonuclease h function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Frauke Christ, Zeger Debyser, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this ...
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Magnesium chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-Diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Zeger Debyser, C. Christ, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this compound on three different viral strains. Experimental data suggest that the antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Dione is probably due to the RNase H inhibition.
Cedric Lion - One of the best experts on this subject based on the ideXlab platform.
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magnesium chelating 2 hydroxyisoquinoline 1 3 2h 4h Diones as inhibitors of hiv 1 integrase and or the hiv 1 reverse transcriptase ribonuclease h domain discovery of a novel selective inhibitor of the ribonuclease h function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Frauke Christ, Zeger Debyser, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this ...
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Magnesium chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-Diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function
Journal of Medicinal Chemistry, 2011Co-Authors: Muriel Billamboz, Fabrice Bailly, Cedric Lion, Nadia Touati, Herve Vezin, Christina Calmels, Marieline Andreola, Zeger Debyser, C. Christ, Philippe CotelleAbstract:2-Hydroxyisoquinoline-1,3(2H,4H)-Dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction with Mg2+ and Mn2+ using different spectroscopic techniques and report that 2-hydroxyisoquinoline-1,3(2H,4H)-Dione forms a 1:1 complex with Mg2+ but a 1:2 complex with Mn2+. The complex formation requires enolization of the ligand. ESR spectroscopy shows a redox reaction between the ligand and Mn2+ producing superoxide anions. Second, 2-hydroxyisoquinoline-1,3(2H,4H)-Dione, its magnesium complex, and its 4-methyl and 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Diones were tested as inhibitors of HIV-1 integrase, reverse transcriptase ribonuclease H, and DNA polymerase functions. Their antiviral activities were evaluated and 2-hydroxy-4-methoxycarbonyl-isoquinoline-1,3(2H,4H)-Dione was found to inhibit the viral replication of HIV-1 in MT-4 cells. Cross-resistance was measured for this compound on three different viral strains. Experimental data suggest that the antiviral activity of 2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-Dione is probably due to the RNase H inhibition.
