Page last updated: 2024-12-08
dioxolane-thymine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
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Protein Interactions
Research Growth
Market Indicators
Description
dioxolane-thymine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 451593 |
| CHEMBL ID | 304445 |
| SCHEMBL ID | 8612207 |
| SCHEMBL ID | 1129570 |
| MeSH ID | M0499146 |
Synonyms (32)
| Synonym |
|---|
| 136982-89-3 |
| (-)-d-.beta.-dioxolane t |
| (-)-1-[(2r,4r)-2-hydroxymethyl)-1,3-dioxan-4-yl]thymine |
| (-)-d-.beta.-dioxolane-thymine |
| DOT , |
| dioxolane-thymine |
| dioxolane thymidine |
| dioxolane t |
| (+/-)-dioxolane-t |
| 2,4(1h,3h)-pyrimidinedione, 1-[(2r,4r)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-5-methyl- |
| (+/-)-dot |
| (+/-)-1-[(2beta,4beta)-2-(hydroxymethyl)-4-dioxolanyl] thymine |
| 1-[(2r,4r)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]-5-methyl-pyrimidine-2,4-dione |
| beta-d-dioxolane thymine |
| CHEMBL304445 |
| (-)-1-((2r,4r)-2-(hydroxymethyl)-1,3-dioxan-4-yl)thymine |
| wt6gzm4ya8 , |
| (-)-d-beta-dioxolane-thymine |
| (-)-d-beta-dioxolane t |
| (+-)-dot |
| 2,4(1h,3h)-pyrimidinedione, 1-((2r,4r)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl- |
| unii-wt6gzm4ya8 |
| (+-)-1-((2beta,4beta)-2-(hydroxymethyl)-4-dioxolanyl) thymine |
| (+-)-dioxolane-t |
| SCHEMBL8612207 |
| SCHEMBL1129570 |
| 4-hydroxy-1-[2-(hydroxymethyl)-1,3-dioxolan-4-yl]-5-methylpyrimidin-2(1h)-one |
| DTXSID90925930 |
| BCAWWPAPHSAUQZ-RNFRBKRXSA-N |
| (-)-1-[(2r,4r)-2-(hydroxymethyl)-4-dioxolanyl]thymine |
| 2,4(1h,3h)-pyrimidinedione, 1-(2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-, (2r-cis)- |
| 1-((2r,4r)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methylpyrimidine-2,4(1h,3h)-dione |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " The pharmacokinetic profiles of D-DOT in serum and urine were adequately described by a two-compartment open pharmacokinetic model." | ( Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. Asif, G; Chu, CK; Delinsky, D; Hurwitz, SJ; McClure, HM; Narayanasamy, J; Obikhod, A; Schinazi, RF, 2007) | 0.34 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (39)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID369078 | Antiviral activity against HIV1 LAI infected in CEM cells | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID406035 | AUC in rhesus monkey at 33.3 mg/kg, po | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406040 | Tlag in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID152650 | Cytotoxicity in peripheral blood mononuclear cells(PBM). | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11 | Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID406044 | Drug elimination in rhesus monkey assessed as beta-dioxolane-thymine-glucuronide elimination at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406039 | Oral bioavailability in rhesus monkey at 33.3 mg/kg | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406031 | Volume of distribution at steady state in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406038 | Cmax in rhesus monkey at 33.3 mg/kg, po | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406043 | Drug elimination in rhesus monkey assessed as beta-dioxolane-thymine-glucuronide elimination at 33.3 mg/kg, po | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406024 | Antiviral activity against Lamivudine resistant HIV1 with reverse transcriptase M184V mutation in human PBMC | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406057 | Drug elimination in monkey urine after 30 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406025 | Antiviral activity against tenofovir resistant HIV1 with reverse transcriptase K65R mutation in human PBMC | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID369081 | Cytotoxicity against african green monkey Vero cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID406032 | AUC in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406034 | Renal clearance in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406046 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, iv after 2 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406045 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, iv after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406028 | Systemic clearance in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406026 | Antiviral activity against didanosine resistant HIV1 with reverse transcriptase L74V mutation in human PBMC | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406048 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, po after 2 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406060 | Ratio of drug level in cerebrospinal fluid to plasma of rhesus monkey at 33.3 mg/kg, po after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406033 | Mean residence time in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406058 | Ratio of drug level in cerebrospinal fluid to plasma of rhesus monkey at 33.3 mg/kg, iv after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406029 | Central volume of distribution in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID369079 | Cytotoxicity against human PBM cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID406042 | Biodistribution in in rhesus monkey urine assessed as dose recovered unchanged at 33.3 mg/kg, iv after 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406037 | Tmax in rhesus monkey at 33.3 mg/kg, po | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406047 | Drug level in rhesus monkey cerebrospinal fluid at 33.3 mg/kg, po after 1 hr | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID229224 | Cytotoxicity in vero cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11 | Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID406036 | Mean residence time in rhesus monkey at 33.3 mg/kg, po | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406059 | Ratio of drug level in cerebrospinal fluid to plasma of rhesus monkey at 33.3 mg/kg, iv after 2 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406023 | Antiviral activity against HIV1 | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406041 | Biodistribution in in rhesus monkey urine assessed as dose recovered unchanged at 33.3 mg/kg, po after 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID154973 | Effective concentration against HIV-1 in peripheral blood mononuclear cells(PBM). | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11 | Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID369080 | Cytotoxicity against human CEM cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID406061 | Ratio of drug level in cerebrospinal fluid to plasma of rhesus monkey at 33.3 mg/kg, po after 2 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID154934 | Effective concentration against HIV-1 strain LAV in human peripheral blood mononuclear (PBM) cells. | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5 | L-beta-(2S,4S)- and L-alpha-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships. |
| AID406030 | Terminal phase half life in rhesus monkey at 33.3 mg/kg, iv | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID406027 | Antiviral activity against zidovudine resistant HIV1 in human PBMC | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (7)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (28.57) | 18.2507 |
| 2000's | 4 (57.14) | 29.6817 |
| 2010's | 1 (14.29) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.41
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.41) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||