Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.

@article{Holloway2009TrypanothioneRH,
  title={Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.},
  author={Georgina A Holloway and William Neil Charman and Alan H. Fairlamb and Reto Brun and M Kaiser and Edmund S. Kostewicz and Patrizia M Novello and John P. Parisot and J. Richardson and Ian P. Street and Keith G Watson and Jonathan B. Baell},
  journal={Antimicrobial agents and chemotherapy},
  year={2009},
  volume={53 7},
  pages={2824-33}
}
High-throughput screening of 100,000 lead-like compounds led to the identification of nine novel chemical classes of trypanothione reductase (TR) inhibitors worthy of further investigation. Hits from five of these chemical classes have been developed further through different combinations of preliminary structure-activity relationship rate probing and assessment of antiparasitic activity, cytotoxicity, and chemical and in vitro metabolic properties. This has led to the identification of novel… CONTINUE READING

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