Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact

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Abstract

Neurokinin-3 receptor (NK3R) plays a pivotal role in the release of gonadotropin-releasing hormone in the hypothalamus–pituitary–gonadal (HPG) axis. To develop novel NK3R antagonists with less environmental toxicity, a series of heterocyclic scaffolds for the triazolopiperazine substructure in an NK3R antagonist fezolinetant were designed and synthesized. An isoxazolo[3, 4–c]piperidine derivative exhibited moderate NK3R antagonistic activity and favorable properties that were decomposable under environmental conditions.

Journal

  • Bioorganic and Medicinal Chemistry

    Bioorganic and Medicinal Chemistry 27(10), 2019-2026, 2019-05-15

    Elsevier Ltd

Codes

  • NII Article ID (NAID)
    120006621580
  • Text Lang
    ENG
  • Article Type
    journal article
  • ISSN
    0968-0896
  • Data Source
    IR 
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