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Title: Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact
Authors: Yamamoto, Koki
Inuki, Shinsuke
Ohno, Hiroaki
Oishi, Shinya
Author's alias: 井貫, 晋輔
大野, 浩章
大石, 真也
Keywords: Environmental impact
Fezolinetant
GnRH
NK3 receptor
Scaffold hopping
Issue Date: 15-May-2019
Publisher: Elsevier Ltd
Journal title: Bioorganic and Medicinal Chemistry
Volume: 27
Issue: 10
Start page: 2019
End page: 2026
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/.
The full-text file will be made open to the public on 15 May 2021 in accordance with publisher's 'Terms and Conditions for Self-Archiving'.
This is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。
URI: http://hdl.handle.net/2433/241057
DOI(Published Version): 10.1016/j.bmc.2019.03.059
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