Synthesis and in vitro antikinetoplastid activity of polyamine-hydroxybenzotriazole conjugates.

@article{Jagu2017SynthesisAI,
  title={Synthesis and in vitro antikinetoplastid activity of polyamine-hydroxybenzotriazole conjugates.},
  author={Elodie Jagu and S{\'e}bastien Pomel and Alba Diez-Martinez and Florence Ramiandrasoa and R. Luise Krauth-Siegel and St{\'e}phanie P{\`e}the and Casimir Blonski and Rapha{\"e}l Labru{\`e}re and Philippe Marie Loiseau},
  journal={Bioorganic & medicinal chemistry},
  year={2017},
  volume={25 1},
  pages={84-90}
}
Thirteen new polyamine derivatives coupled to hydroxybenzotriazole have been synthesized and evaluated for their in vitro antikinetoplastid activity. Trypanosoma Trypanothione reductase (TryR) was envisioned as a potential target. Among all tested molecules, only one compound, a N3-spermidine-benzotriazole derivative, displayed relevant inhibitory activity… CONTINUE READING