Dihydrofolate reductase inhibitors: New developments in antiparasitic chemotherapy

Expert Opinion on Therapeutic Patents

Volumn 11, Issue 8, 2001, Pages 1285-1290

  Durand, R ^a   Savel, J ^a  

^a BICHAT HOSPITAL   (France)

Author keywords

DHFR; Dihydrofolate reductase inhibitors; Neospora; Plasmodium; Pneumocystis; Toxoplasma

Indexed keywords

2,4 DIAMINO 6 (2 NAPHTHYLSULFONYL)QUINAZOLINE; 2,4 DIAMINOPYRIMIDINE DERIVATIVE; 4,6 DIAMINO 1,2 DIHYDRO 2,2 DIMETHYL 1 [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] 1,3,5 TRIAZINE; ANTIMALARIAL AGENT; ANTIPARASITIC AGENT; ATOVAQUONE; ATOVAQUONE PLUS PROGUANIL; CHLORPROGUANIL; CYCLOGUANIL; DAPSONE; DIHYDROFOLATE REDUCTASE INHIBITOR; DIHYDROPTEROATE SYNTHASE; EPIROPRIM; HALOFANTRINE; LAP DAP; MEFLOQUINE; METHOTREXATE; N [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] N' ISOPROPYLIMIDOCARBONIMIDIC DIAMIDE; PIRITREXIM; PRIMAQUINE; PROGUANIL; PYRIMETHAMINE; QUINAZOLINE DERIVATIVE; SULFADOXINE; SULFAFURAZOLE; SULFAMETHOXAZOLE; SULFONAMIDE; TRIMETHOPRIM; TRIMETREXATE; TRIMETREXATE GLUCURONATE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANTIBIOTIC PROPHYLAXIS; ANTIBIOTIC RESISTANCE; ANTIMICROBIAL ACTIVITY; CONTROLLED STUDY; DRUG EFFICACY; DRUG STRUCTURE; HUMAN; MALARIA; NEOSPORA CANINUM; PATENT; PLASMODIUM FALCIPARUM; PNEUMOCYSTIS PNEUMONIA; REVIEW; TOXOPLASMOSIS;

EID: 0034908668     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.11.8.1285     Document Type: Review

References (44)

1. Folate metabolism in malaria
2. Intrinsic and acquired resistance to methotrexate in acute leukemia
3. Methotrexate transport and resistance
4. Spread of chloroquine resistance in Plasmodium falciparum
5. Increased incidence of cycloguanil resistance in malaria cases entering France from Africa, determined as point mutations in the parasites' dihydrofolate-reductase genes
6. PS-15: A potent, orally active antimalarial from a new class of folic acid antagonists
7. The antimalarial triazine WR99210 and the prodrug PS-15: Folate reversal of in vitro activity against Plasmodium falciparum and a non-antifolate mode of action of the prodrug
8. Analysis in yeast of antimalarial drugs that target the dihydrofolate reductase of Plasmodium falciparum
9. Synergistic antimalarial activity of dapsone/dihydrofolate reductase inhibitors and the interaction of antifol, antipyrimidine and antipurine combinations against Plasmodium falciparum in vitro
10. In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocytes CFUs
11. Chloproguanildapsone: Effective treatment for uncomplicated falciparum malaria
12. Malarone (atovaquone and proguanil hydrochloride): A review of its clinical development for treatment of malaria
13. New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii
14. Evaluation of potent inhibitors of dihydrofolate reductase in a culture model for growth of Pneumocystis carinii
15. Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim
16. 6-Substituted 2,4-diaminopyrido[3,2d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocysis carinii, and iand as antitumor agents
17. Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase antitumor agents: Synthesis and biological activities of 2,4- diamino- methyl] pyrido [2,3-d] pyrimidines
18. Inhibition of dihydrofolate reductases from Toxoplasma gondii, Pneumocystis carinii, and rat liver by rotationally restricted analogues of pyrimethamine and metoprine
19. Rational drug design approach for overcoming drug resistance: Application to pyrimethamine resistance in malaria
20. High-affinity inhibitors of dihydrofolate reductase: Antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size
21. Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase
22. Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: Activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents
23. Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase
24. Combination of PS-15, epiroprim, or pyrimethamine with dapsone in prophylaxis of Toxoplasma gondii and Pneumocystis carinii dual infection in a rat model
25. Efficacy of epiroprim (Ro 11-8958), a new dihydrofolate reductase inhibitor, in the treatment of acute Toxoplasma infection in mice
26. Activity of Epiroprim (Ro 11-8958), a dihydrofolate reductase inhibitor, alone and in combination with dapsone against Toxoplasma gondii
27. Neosporosis
28. Demonstration of synergistic effects of sulfonamides and dihydrofolate reductase/thymidylate synthase inhibitors against Neospora caninum tachyzoites in cultured cells, and characterization of mutants resistant to pyrimethamine
29. Cruzipain, the major cysteine proteinase from the protozoan parasite Trypanosoma cruzi
30. Cysteine protease inhibitors as chemotherapy for parasitic infections
31. Development of cysteine protease inhibitors as chemotherapy for parasitic diseases: Insights on safety, target validation, and mechanism of action
32. Parasite proteinases and amino acid metabolism: Possibilities for chemotherapeutic exploitation
33. Proteases of malaria parasites: New targets for chemotherapy
34. ATP-site directed inhibitors of cyclin-dependent kinases
35. Properties and potential applications of chemical inhibitors of cyclin-dependent kinases
36. Ribonucleotide reductase: A new target for antiparasitic therapies
37. Lipid biosynthesis pathways as chemotherapeutic targets in kinetoplastid parasites
38. Short-course treatment of visceral leishmaniasis with liposomal amphotericin B
39. Amino acid changes linked to pyrimethamine resistance in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum
40. Evidence that a point mutation in dihydrofolate reductase-thymidylate synthase confers resistance to pyrimethamine in falciparum malaria
41. The dihydrofolate reductase-thymidylate synthetase gene in the drug resistance of malaria parasites
42. Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria
43. Point mutations in the dihydrofolate reductase-thymidylate synthase gene and pyrimethamine and cycloguanil resistance in Plasmodium falciparum
44. Preventing antimalarial drug resistance through combinations