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Keywords:

  • dihydropyrimidones;
  • inhibitors;
  • membrane proteins;
  • sodium iodide symporter;
  • structure–activity relationships
Thumbnail image of graphical abstract

The front cover picture shows the structure of a new dihydropyrimidin-2-one inhibitor of iodide entrapment in thyroid cells. The identification of this low-nanomolar inhibitor was achieved through an exhaustive structure–activity relationship study in which more than a hundred derivatives in this compound family were designed, synthesized and tested. This discovery opens new perspectives for the development of antithyroid drugs designed to prevent iodide overload in the thyroid gland. For more details, see the Full Paper by Yves Ambroise et al. on p. 104 ff.