Structure-Based Design of Pteridine Reductase Inhibitors Targeting African Sleeping Sickness and the Leishmaniases†

@inproceedings{Tulloch2010StructureBasedDO,
  title={Structure-Based Design of Pteridine Reductase Inhibitors Targeting African Sleeping Sickness and the Leishmaniases†},
  author={Lindsay B Tulloch and Viviane Paula Martini and Jorge Iulek and Judith K. Huggan and Jeong Hwan Lee and Colin L. Gibson and Terry K. Smith and Colin J. Suckling and William N. Hunter},
  booktitle={Journal of medicinal chemistry},
  year={2010}
}
Pteridine reductase (PTR1) is a target for drug development against Trypanosoma and Leishmania species, parasites that cause serious tropical diseases and for which therapies are inadequate. We adopted a structure-based approach to the design of novel PTR1 inhibitors based on three molecular scaffolds. A series of compounds, most newly synthesized, were identified as inhibitors with PTR1-species specific properties explained by structural differences between the T. brucei and L. major enzymes… CONTINUE READING