BDBM50370476 ZIDOVUDINE TRIPHOSPHATE Combivir
AZIDOTHYMIDINE MONOPHOSPHATE BDBM50478975 Zidovudine Monophosphate
1-((2R,4S,5S)-4-(diazoamino)-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione Retrovir 3'-Deoxy-3-azidothymidine 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione (AZT) US10071110, Compound AZT 1-((2R,4S,5S)-4-azido-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione 1-((2R,4S,5S)-4-azido-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione 3'-azido-thymidine 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione (N3ddThd) 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione(Zidovudine, AZT) zudovidine 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione(3'-azido-2',3'-dideoxythymidine) 1-((2R,5S)-4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione (AzddThd, AZT) 3'-azido-2',3'-dideoxythymidine BWA509U 1-((2R,4R,5S)-4-azido-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione(AZT) 3-((2S,3S,5R)-2-(hydroxymethyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-3-yl)triaz-1-en-2-ium-1-ide 1-((2R,4S,5S)-4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione US11420959, Example AZT (AZT)1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione azidothymidine 1-((2S,4R,5R)-4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione ZIDOVUDINE 3'-Azido-3'-deoxy-thymidine zidovudin CHEMBL129 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione(azidothymidine, AZT) 4-(4-Azido-5-hydroxy-tetrahydro-furan-2-yl)-5-methyl-3H-pyrazine-2,6-dione 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione [AZT] BW-A-509U AZT BDBM50002692 3'azido-2'3'-dideoxythymidine (AZT) 1-(4-Azido-5-hydroxymethyl-tetrahydro-furan-2-yl)-5-methyl-1H-pyrimidine-2,4-dione
- ChEMBL_1488942 (CHEMBL3535608) Uncompetitive substrate inhibition of UGT2B7 in diabetic human liver microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method
- ChEMBL_1488946 (CHEMBL3535612) Uncompetitive substrate inhibition of UGT2B7 in diabetic human kidney microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method
- ChEMBL_1493710 (CHEMBL3530459) Uncompetitive substrate inhibition of UGT2B7 in non-diabetic human liver microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method
- ChEMBL_1493714 (CHEMBL3530463) Uncompetitive substrate inhibition of UGT2B7 in non-diabetic human kidney microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method
- ChEMBL_583934 (CHEMBL1061785) Binding affinity to wild type HIV1 LAI reverse transcriptase assessed as ATP-mediated excision of zidovudine-monophosphate terminated DNA/DNA template/primer duplex chain at 100 uM by gel shift mobility assay
- ChEMBL_583935 (CHEMBL1061786) Binding affinity to HIV1 LAI reverse transcriptase M184V mutant assessed as ATP-mediated excision of zidovudine-monophosphate terminated DNA/DNA template/primer duplex chain at 100 uM by gel shift mobility assay
- ChEMBL_583936 (CHEMBL1061787) Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y mutant assessed as ATP-mediated excision of zidovudine-monophosphate terminated DNA/DNA template/primer duplex chain at 100 uM by gel shift mobility assay
- ChEMBL_583937 (CHEMBL1061788) Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V mutant assessed as ATP-mediated excision of zidovudine-monophosphate terminated DNA/DNA template/primer duplex chain at 100 uM by gel shift mobility assay
- ChEMBL_583943 (CHEMBL1062617) Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/K65R mutant assessed as ATP-mediated excision of zidovudine-monophosphate terminated DNA/DNA template/primer duplex chain at 100 uM by gel shift mobility assay
- HIV-1 plaque reduction assay Preliminary experiments in the inhibition of HIV-1 replication by invention compounds were performed as follows. Drug assays were carried out as previously described by Larder et. al., Antimicrobial Agents & Chemotherapy, 34:436-441, 1990. HIV-1LA1 infected HT4-6C cells were exposed to drugs as indicated and incubated for 3 days at 37° C. The cells were fixed with crystal violet to visualize plaques. Antiviral activity was assessed as the percentage of control plaques (no drug) measured in drug treated samples. The EC50 is the micromolar concentration which reduces plaque number by 50%. The activity of adefovir was compared with AZT (zidovudine) and 1-O-hexadecylpropanediol-3-adefovir (HDP-ADV) in HIV-1 infected HT4-6C cells.
- Anti-HIV-1 Activity Test C8166 cells infected with HIV-1 were used for determining the anti-HIV biological activity at the cellular level. The specific method was described below.Cytotoxicity experiment: The toxicity of the compounds on C8166 cells was determined by MTT method. In a 96-well cell culture plate, the compounds were subjected to 5-fold serial dilution and 100 μL of C8166 cell suspension (4×105/mL) was added into each well. Three replicate wells were set for each concentration. At the same time, a cell control group without drugs and drug control groups with Zidovudine (AZT) or Nevirapine (NVP) were set. The cells were incubated at 37° C. in a 5% CO2 incubator for three days, followed by the addition of MTT solution into each well, and then the cells were incubated at 37° C. for 4 hours. 15% SDS-50% DMF was added to each well and the cells were incubated at 37° C. in a 5% CO2 incubator overnight. After mixing evenly, the OD values were measured by BIO-TEK ELx800 ELISA instrument (determination wavelength: 570 nm; reference wavelength: 630 nm). The dose-response curve was graphed according to the experimental results, and the CC50 was calculated (the concentrations of the compounds required to produce toxicity on 50% cells).Syncytium inhibition experiment: 100 μL of C8166 cell suspension (4×105/mL) was inoculated into each well of a 96-well cell culture plate containing 5-fold serial dilutions of the compounds, followed by addition of HIV-1IIIB diluted supernatant (MOI=0.04). Three replicate wells were set for each serial concentration. At the same time, negative control wells of HIV-1IIIB infection without compounds and positive control wells with Zidovudine (AZT) or Nevirapine (NVP) were set. The cells were incubated at 37° C. in a 5% CO2 incubator for three days. The number of the syncytia was counted in five non-overlapping fields of view by using an inverted microscope (100×). The dose-response curves were graphed according to the experimental results, and the 50% effective concentrations of the compounds for inhibiting the virus (EC50, 50% effective concentration) were calculated according to Reed & Muench method. Calculation formula: cytopathic inhibition rate (%)=(1−number of syncytia in experimental wells/number of syncytia in control well)×100%.