Desazadesmethyldesferrithiocin analogues as orally effective iron chelators.

@article{Bergeron1999DesazadesmethyldesferrithiocinAA,
  title={Desazadesmethyldesferrithiocin analogues as orally effective iron chelators.},
  author={Raymond J. Bergeron and Jan Wiegand and William R. Weimar and J. R. Timothy Vinson and Joerg Bussenius and Guocan Yao and James S. McManis},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 1},
  pages={95-108}
}
Further structure-activity studies of desferrithiocin analogues are carried out. (S)-Desazadesmethyldesferrithiocin, 2-(2-hydroxyphenyl)-Delta2-thiazoline-4(S)-carboxylic acid, serves as the principal framework in the current paper. Desazadesmethyldesferrithiocin can be structurally altered with facility, and data are already available on its iron-clearing properties and toxicity parameters. Four different kinds of structural modifications of this framework are undertaken: introduction of… CONTINUE READING

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PrimatesNo subtypeRodent
Ligands with efficiencies greater than 3% in the primate are then evaluated in a formal toxicity study in rodents .
RodentNo subtypePrimates
Ligands with efficiencies greater than 3% in the primate are then evaluated in a formal toxicity study in rodents .
Four different kinds of structural modifications of this framework are undertaken : introduction of hydroxy , carboxy , or methoxy groups on the aromatic ring ; alteration of the thiazoline ring ; increasing the distance between the ligand donor atoms ; and benz - fusion of the aromatic rings .
Four different kinds of structural modifications of this framework are undertaken : introduction of hydroxy , carboxy , or methoxy groups on the aromatic ring ; alteration of the thiazoline ring ; increasing the distance between the ligand donor atoms ; and benz - fusion of the aromatic rings .
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