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Keywords:

  • benzamides;
  • cognitive disorders;
  • histamine H3 receptors;
  • structure–activity relationships;
  • thiazoles
Thumbnail image of graphical abstract

The simpler, the better: H3 histamine receptor (H3R) are of interest as therapeutic targets in cognitive and somnolence disorders. Here, lead optimization of H3R inverse agonists bearing a thiazolo[5,4-c]piperidine group gave rise to a clinical candidate with a much simpler unprecedented benzamide scaffold, displaying decreased hERG activity while maintaining high brain receptor occupancies.