Development Of Nk3r Antagonists With A Degradable Scaffold In The Natural Environment: Identification Of Nk3r Antagonists With A Decomposable Core Structure By Scaffold Hopping

For development of novel NK3R antagonists with less environmental toxicity, a series of heterocyclic scaffolds for the triazolopiperazine substructure in fezolinetant were designed and synthesized. An isoxazolo[3,4-c]piperidine derivative exhibited moderate NK3R antagonistic activity with the favorable properties decomposable under environmental conditions.