Page last updated: 2024-08-07 15:24:09
Dihydrofolate reductase
[no definition available]
Synonyms
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (7.69) | 18.2507 |
| 2000's | 10 (76.92) | 29.6817 |
| 2010's | 2 (15.38) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (6)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| trimethoprim | Mycobacterium avium | IC50 | 33.5633 | 9 | 9 |
| trimetrexate | Mycobacterium avium | IC50 | 0.3012 | 5 | 5 |
| piritrexim | Mycobacterium avium | IC50 | 0.0006 | 5 | 5 |
| epiroprim | Mycobacterium avium | IC50 | 0.0041 | 1 | 1 |
| sori 8895 | Mycobacterium avium | IC50 | 0.0011 | 1 | 1 |
| sori 8890 | Mycobacterium avium | IC50 | 0.0200 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| trimethoprim | Mycobacterium avium | Activity | 0.3000 | 1 | 1 |
| sori 8895 | Mycobacterium avium | Activity scale | 0.0100 | 1 | 1 |
| sori 8890 | Mycobacterium avium | Activity scale | 0.0100 | 1 | 1 |
Design, synthesis, biological evaluation and computational investigation of novel inhibitors of dihydrofolate reductase of opportunistic pathogens.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivityJournal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
Design, synthesis, and biological evaluation of 2,4-diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 14, Issue:7, 2004
New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003