Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact
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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.
- Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry 27(10), 2019-2026, 2019-05-15