Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact

Yamamoto, Koki; Inuki, Shinsuke; Ohno, Hiroaki; Oishi, Shinya

ダウンロード数: 245

http://hdl.handle.net/2433/241057

このアイテムのファイル:

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

完全メタデータレコード

DCフィールド	値	言語
dc.contributor.author	Yamamoto, Koki	en
dc.contributor.author	Inuki, Shinsuke	en
dc.contributor.author	Ohno, Hiroaki	en
dc.contributor.author	Oishi, Shinya	en
dc.contributor.alternative	井貫, 晋輔	ja
dc.contributor.alternative	大野, 浩章	ja
dc.contributor.alternative	大石, 真也	ja
dc.date.accessioned	2019-04-26T05:52:08Z	-
dc.date.available	2019-04-26T05:52:08Z	-
dc.date.issued	2019-05-15	-
dc.identifier.issn	0968-0896	-
dc.identifier.issn	1464-3391	-
dc.identifier.uri	http://hdl.handle.net/2433/241057	-
dc.description.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.	en
dc.format.mimetype	application/pdf	-
dc.language.iso	eng	-
dc.publisher	Elsevier BV	en
dc.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/.	en
dc.rights	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'.	en
dc.rights	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。	ja
dc.rights	This is not the published version. Please cite only the published version.	en
dc.subject	Environmental impact	en
dc.subject	Fezolinetant	en
dc.subject	GnRH	en
dc.subject	NK3 receptor	en
dc.subject	Scaffold hopping	en
dc.title	Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact	en
dc.type	journal article	-
dc.type.niitype	Journal Article	-
dc.identifier.ncid	AA10938083	-
dc.identifier.jtitle	Bioorganic & Medicinal Chemistry	en
dc.identifier.volume	27	-
dc.identifier.issue	10	-
dc.identifier.spage	2019	-
dc.identifier.epage	2026	-
dc.relation.doi	10.1016/j.bmc.2019.03.059	-
dc.textversion	author	-
dc.address	Graduate School of Pharmaceutical Sciences, Kyoto University	en
dc.address	Graduate School of Pharmaceutical Sciences, Kyoto University	en
dc.address	Graduate School of Pharmaceutical Sciences, Kyoto University	en
dc.address	Graduate School of Pharmaceutical Sciences, Kyoto University	en
dc.identifier.pmid	30975505	-
dcterms.accessRights	open access	-
datacite.date.available	2021-05-15	-
datacite.awardNumber	17J10582	-
dc.identifier.pissn	0968-0896	-
jpcoar.funderName	日本学術振興会	ja
jpcoar.funderName.alternative	Japan Society for the Promotion of Science (JSPS)	en
出現コレクション:	学術雑誌掲載論文等

アイテムの簡略レコードを表示する

Export to RefWorks

このリポジトリに保管されているアイテムはすべて著作権により保護されています。