Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact-Science-Chemical Encyclopedia-lookchem

Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact
Add time:07/11/2019 Source:sciencedirect.com

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.

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