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The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase
- Source :
- Bioorganicmedicinal chemistry letters. 9(10)
- Publication Year :
- 1999
-
Abstract
- This paper describes the design and synthesis of potential inhibitors of Trypanosoma cruzi dihydrofolate reductase using a structure-based approach. A model of the structure of the T. cruzi enzyme was compared with the structure of the human enzyme. The differences were used to design modifications of methotrexate to produce compounds which should be selective for the parasite enzyme. The derivatives of methotrexate were synthesised and tested against the enzyme and intact parasites.
- Subjects :
- Trypanosoma cruzi
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Cell Line
chemistry.chemical_compound
Mice
parasitic diseases
Drug Discovery
Dihydrofolate reductase
medicine
Animals
Humans
Binding site
Enzyme Inhibitors
Amastigote
Molecular Biology
chemistry.chemical_classification
Binding Sites
biology
Molecular Structure
Organic Chemistry
biology.organism_classification
Recombinant Proteins
Tetrahydrofolate Dehydrogenase
Enzyme
chemistry
Enzyme inhibitor
Drug Design
Antifolate
biology.protein
Molecular Medicine
Folic Acid Antagonists
Methotrexate
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 9
- Issue :
- 10
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....626ca47292372e3e5b56acc5b87a2e8e