Synthesis of N-Alkyl-Carbazole Derivatives as 5-HT7R Antagonists
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kim, Youngjae | - |
dc.contributor.author | Yeom, Miyoung | - |
dc.contributor.author | Lee, Soyeon | - |
dc.contributor.author | Tae, Jinsung | - |
dc.contributor.author | Kim, Hak Joong | - |
dc.contributor.author | Rhim, Hyewhon | - |
dc.contributor.author | Seong, Jihye | - |
dc.contributor.author | Choi, Kyung Il | - |
dc.contributor.author | Min, Sun-Joon | - |
dc.contributor.author | Choo, Hyunah | - |
dc.date.accessioned | 2021-09-02T07:23:07Z | - |
dc.date.available | 2021-09-02T07:23:07Z | - |
dc.date.created | 2021-06-16 | - |
dc.date.issued | 2018-09 | - |
dc.identifier.issn | 0253-2964 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/73625 | - |
dc.description.abstract | We designed and synthesized a series of N-alkyl-carbazoles with different alkyl chains and amine moieties, and biological evaluation was performed to discover novel 5-HT7R antagonists. Among 27 synthesized compounds, 20, 21, 23, and 24 showed excellent binding affinities to 5-HT7R (K-i = 65, 64, 55, and 31 nM, respectively), and good selectivity profiles over other serotonin receptors. In functional assays, those compounds showed weak antagonistic activities against 5-HT7R. In particular, the compound 24, 2-(4-(5-(9H-carbazol-9-yl)pentyl)piperazin-1-yl)phenol, could be considered as a potent and selective 5-HT7R ligand with weak antagonistic effect. From the molecular docking study, the aromatic hydroxyl group in 24 was shown to play an important role in binding to 5-HT7R through a hydrogen bonding interaction with Asp142 in the ligand binding pocket of 5-HT7R. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.subject | ANTIDEPRESSANT-LIKE BEHAVIOR | - |
dc.subject | EYE-MOVEMENT SLEEP | - |
dc.subject | RECEPTOR ANTAGONIST | - |
dc.subject | SEROTONIN RECEPTORS | - |
dc.subject | NEURONAL MORPHOLOGY | - |
dc.subject | DEPRESSION | - |
dc.subject | LIGANDS | - |
dc.subject | BINDING | - |
dc.subject | PHARMACOPHORE | - |
dc.subject | SB-269970 | - |
dc.title | Synthesis of N-Alkyl-Carbazole Derivatives as 5-HT7R Antagonists | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Kim, Hak Joong | - |
dc.identifier.doi | 10.1002/bkcs.11555 | - |
dc.identifier.scopusid | 2-s2.0-85053235534 | - |
dc.identifier.wosid | 000444410200011 | - |
dc.identifier.bibliographicCitation | BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.39, no.9, pp.1083 - 1089 | - |
dc.relation.isPartOf | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.title | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.volume | 39 | - |
dc.citation.number | 9 | - |
dc.citation.startPage | 1083 | - |
dc.citation.endPage | 1089 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.identifier.kciid | ART002384238 | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.subject.keywordPlus | ANTIDEPRESSANT-LIKE BEHAVIOR | - |
dc.subject.keywordPlus | EYE-MOVEMENT SLEEP | - |
dc.subject.keywordPlus | RECEPTOR ANTAGONIST | - |
dc.subject.keywordPlus | SEROTONIN RECEPTORS | - |
dc.subject.keywordPlus | NEURONAL MORPHOLOGY | - |
dc.subject.keywordPlus | DEPRESSION | - |
dc.subject.keywordPlus | LIGANDS | - |
dc.subject.keywordPlus | BINDING | - |
dc.subject.keywordPlus | PHARMACOPHORE | - |
dc.subject.keywordPlus | SB-269970 | - |
dc.subject.keywordAuthor | 5-HT7 receptor | - |
dc.subject.keywordAuthor | Antagonist | - |
dc.subject.keywordAuthor | N-alkyl-carbazole | - |
dc.subject.keywordAuthor | Serotonin | - |
dc.subject.keywordAuthor | GPCR | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
(02841) 서울특별시 성북구 안암로 14502-3290-1114
COPYRIGHT © 2021 Korea University. All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.