Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Identification of NK3R Antagonists with a Decomposable Core Structure by Scaffold Hopping

Part of the Springer Theses book series (Springer Theses)


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.


NK3R antagonist Fezolinetant Scaffold hopping Photodegradation 


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© Springer Nature Singapore Pte Ltd. 2020

Authors and Affiliations

  1. 1.Graduate School of Pharmaceutical SciencesKyoto UniversityKyotoJapan

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