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| ファイル | 記述 | サイズ | フォーマット | |
|---|---|---|---|---|
| j.bmc.2019.03.059.pdf | 397.55 kB | Adobe PDF | 見る/開く |
| タイトル: | Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact |
| 著者: | Yamamoto, Koki Inuki, Shinsuke    https://orcid.org/0000-0002-7525-1280 (unconfirmed)Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed)Oishi, Shinya |
| 著者名の別形: | 井貫, 晋輔 大野, 浩章 大石, 真也 |
| キーワード: | Environmental impact Fezolinetant GnRH NK3 receptor Scaffold hopping |
| 発行日: | 15-May-2019 |
| 出版者: | Elsevier BV |
| 誌名: | Bioorganic & Medicinal Chemistry |
| 巻: | 27 |
| 号: | 10 |
| 開始ページ: | 2019 |
| 終了ページ: | 2026 |
| 抄録: | 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. |
| 著作権等: | © 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'. 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。 This is not the published version. Please cite only the published version. |
| URI: | http://hdl.handle.net/2433/241057 |
| DOI(出版社版): | 10.1016/j.bmc.2019.03.059 |
| PubMed ID: | 30975505 |
| 出現コレクション: | 学術雑誌掲載論文等 |
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