Efficacies of lipophilic inhibitors of dihydrofolate reductase against parasitic protozoa

Antimicrobial Agents and Chemotherapy

Volumn 45, Issue 1, 2001, Pages 187-195

  Lau, H ^a   Ferlan, J T ^a   Brophy, V H ^a   Rosowsky, A ^a   Sibley, C H ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; DIHYDROFOLATE REDUCTASE INHIBITOR; QUINAZOLINE DERIVATIVE; TETRAHYDROQUINAZOLINE DERIVATIVE;

ANTIMALARIAL ACTIVITY; ARTICLE; CRYPTOSPORIDIUM PARVUM; DRUG POTENCY; LIPOPHILICITY; MALARIA; NONHUMAN; PARASITEMIA; PLASMODIUM FALCIPARUM; PNEUMOCYSTIS CARINII; POINT MUTATION; PRIORITY JOURNAL; SACCHAROMYCES CEREVISIAE; TOXOPLASMA GONDII;

ALLELES; ANIMALS; ANTIPROTOZOAL AGENTS; CRYPTOSPORIDIUM PARVUM; DRUG RESISTANCE; FOLIC ACID ANTAGONISTS; HUMANS; LIPIDS; PLASMIDS; PLASMODIUM FALCIPARUM; PNEUMOCYSTIS; PROTOZOA; PYRIMETHAMINE; TETRAHYDROFOLATE DEHYDROGENASE; TOXOPLASMA;

EID: 0035165406     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.45.1.187-195.2001     Document Type: Article

References (49)

1. Molecular epidemiology of malaria in Yaounde, Cameroon I. Analysis of point mutations in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum
2. Eukaryotic dihydrofolate reductase
3. Identification of Cryptosporidium parvum dihydrofolate reductase inhibitors by complementation in Saccharomyces cerevisiae
4. Molecular cloning and sequence analysis of the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene
5. Methotrexate analogs. 6. Replacement of glutamic acid by various amino acid esters and amines
6. Methotrexate analogs. 3. Synthesis and biological properties of some side-chain altered analogs
7. Identification of highly potent and selective inhibitors of Toxoplasma gondii dihydrofolate reductase
8. Observations on monthly pyrimethamine prophylaxis in an East African village
9. The mechanisms of drug action and resistance in malaria
10. Isolation and expression of the Pneumocystis carinii dihydrofolate reductase gene
11. Nucleotide sequence of the dihydrofolate reductase gene of Saccharomyces cerevisiae
12. Inhibition of folate biosynthesis and function as a basis for chemotherapy
13. The phenotype of a dihydrofolate reductase mutant in Saccharomyces cerevisiae
14. In search of dihydrofolate reductase
15. The methotrexate story: A paradigm for development of cancer chemotherapeutic agents
16. The dihydrofolate reductase-thymidylate synthase gene in the drug resistance of malaria parasites
17. Polymorphisms in the dihydrofolate reductase (DHFR) and dihydropteroate synthetase (DHPS) genes of Plasmodium falciparum and in vivo resistance to sulfadoxine/pyrimethamine in isolates from Tanzania
18. 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
19. In vitro activities of and mechanisms of resistance to antifol antimalarial drugs
20. Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples
21. Kenyan Plasmodium falciparum field isolates: Correlation between pyrimethamine and chlorcycloguanil activity in vitro and point mutations in the dihydrofolate reductase domain
22. Community pyrimethamine-sulfadoxine use and prevalence of resistant Plasmodium falciparum genotypes in Mali: A model for deterring resistance
23. Expression and site-directed mutagenesis of human dihydrofolate reductase
24. A biochemical and genetic model for parasite resistance to antifolates. Toxoplasma gondii provides insights into pyrimethamine and cycloguanil resistance in Plasmodium falciparum
25. Pteridines. 2. New 6,7-disubstituted pteridines as potential antimalarial and antitumor agents
26. Structure-based design of selective inhibitors of dihydrofolate reductase: Synthesis and antiparasitic activity of 2,4-diaminopteridine analogues with a bridged diarylamine side chain
27. Methotrexate analogs. 8. Synthesis and biological evaluation of bisamide derivatives of potential prodrugs
28. 2,4-Diaminopyrido[3,2-d]pyrimidine inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii
29. Chemical and biological studies on dihydro-s-triazines. XVI. NMR evidence for the formation of 2-guanidino-4-methylquinazolines as anomalous byproducts in the three-component synthesis
30. Brominated trimetrexate analogues as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase
31. Synthesis and antifolate activity of 2,4-diamino-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine analogues of trimetrexate and piritrexim
32. 2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii
33. 2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase
34. 2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: Synthesis and antifolate activity
35. Chemical and biological studies on dihydro-s-triazines. XVII. Modifications of the three-component synthesis favoring the formation of 2-guanidino-4-methylquinazoline byproducts
36. Synthesis and antiparasitic and antitumor activity of 2,4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim
37. 2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase
38. 2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase
39. One-step synthesis of novel 2,4-diaminopyrimidine antifolates from bridged alicyclic ketones and cyanognanidine
40. Analogs of pteroylglutamic acid. III. 4-Amino derivatives
41. Yeast as a model system to study drugs effective against apicomplexan proteins
42. A system of shuttle vectors and yeast host strains designed for efficient manipulation of DNA in Saccharomyces cerevisiae
43. Potential antifolate resistance determinants and genotypic variation in the bifunctional dihydrofolate reductase-thymidylate synthase gene from human and bovine isolates of Cryptosporidium parvum
44. Resistance to antifolates in Plasmodium falciparum monitored by sequence analysis of dihydropteroate synthetase and dihydrofolate reductase alleles in a large number of field samples of diverse origins
45. Analysis in yeast of antimalaria drugs that target the dihydrofolate reductase of Plasmodium falciparum
46. Chemotherapy and immunity in opportunistic parasitic infections in AIDS