The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Article Details
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Zuccotto F, Brun R, Gonzalez Pacanowska D, Ruiz Perez LM, Gilbert IH
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Bioorg Med Chem Lett. 1999 May 17;9(10):1463-8.
- PubMed ID
- 10360757 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Methotrexate Dihydrofolate reductase Ki (nM) 0.179 N/A N/A Details Methotrexate Dihydrofolate reductase Ki (nM) 0.038 N/A N/A Details