Synthesis of novel nucleosides of 4-oxoquinoline-3-carboxylic acid analogues

Abstract

A series of new ribonucleosides 1a–d having 4‐oxoquinoline‐3‐carboxylic acid substituted with a chloro or bromo atom in the aromatic ring, as the nitrogen base, was synthesized and examined for anti‐HIV activity. Compounds 1a and 1c showed a modest inhibition activity on HIV‐1 reverse transcriptase, inhibiting 10% of the enzyme activity at the concentration of 100 μM. © 1999 John Wiley & Sons, Inc. Heteroatom Chem 10: 197–202, 1999

Inhibition of HIV-1 Replication in Human Primary Cells by a Dolabellane Diterpene Isolated from the Marine AlgaeDictyota pfaffii

“…The inhibitory effect of compound 3 on RT polymerase activity was evaluated using unpurified and purified recombinant HIV-1 RT enzymes, as reported [18]. In summary, the polymerization reactions contained 50 mM Tris HCl (pH 7.8), 6 mM MgCl 2 , 1 mM dithiothreitol, 50 mM KCl, 20 mM dTTP, 10 mM of [ 3 H]dTTP (47 Ci/mmol), and 150 mg /mL poly(rA) oligo(dT) template primer (Pharmacia) and 1 U of enzyme (defined as the amount of enzyme that incorporates 1 pmol of dTTP in 30 min at 37 8C under standard assay conditions).…”

Anti-HIV-1 Activity of theIbogaAlkaloid Congener 18-Methoxycoronaridine

“…Viral replication was measured as for infected PBMCs. Anti-HIV-1 reverse transcriptase (RT) inhibitory activity The inhibitory effect of 18-MC on the RT polymerase activity was evaluated using recombinant HIV-1 RT, obtained as previously described [16]. The polymerization reactions contained 50 mM Tris HCl (pH 7.8), 6 mM MgCl 2 , 1 mM dithiothreitol, 50 mM KCl, 20 mM dTTP, 10 mM of [ 3 H]dTTP (47 Ci/mmol), and 150 mg/mL poly(rA) oligo(dT) template primer (Pharmacia) and 1 U of enzyme (defined as the amount of enzyme that incorporates 1 pmol of dTTP in 30 min at 37 8C under standard assay conditions).…”

Characterization of HIV-1 Enzyme Reverse Transcriptase Inhibition by the Compound 6-Chloro-1,4-Dihydro-4-Oxo-1-(β-D-Ribofuranosyl) Quinoline-3-Carboxylic Acid Through Kinetic and In Silico Studies

“…To analyze the dTTP incorporation, saturating concentrations of poly(rA)o(dT) [12][13][14][15][16][17][18] (100 nM) and various concentrations of dTTP (ranging from 0 -30 μM) were added to buffer A. Inversely, to analyze the TP uptake, a saturating concentration of dTTP (60 μM) and various concentrations of poly(rA)o(dT) [12][13][14][15][16][17][18] (ranging from 0 -100 nM) were added to buffer A. To analyze the dTTP incorporation, saturating concentrations of poly(rA)o(dT) [12][13][14][15][16][17][18] (100 nM) and various concentrations of dTTP (ranging from 0 -30 μM) were added to buffer A. Inversely, to analyze the TP uptake, a saturating concentration of dTTP (60 μM) and various concentrations of poly(rA)o(dT) [12][13][14][15][16][17][18] (ranging from 0 -100 nM) were added to buffer A.…”