|Title:||Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact|
Inuki, Shinsuke https://orcid.org/0000-0002-7525-1280 (unconfirmed)
Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed)
|Author's alias:||井貫, 晋輔|
|Journal title:||Bioorganic & medicinal chemistry|
|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.|
|Rights:||© 2019. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/.|
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|Appears in Collections:||Journal Articles|
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