Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 민선준 | - |
dc.date.accessioned | 2019-05-31T02:17:46Z | - |
dc.date.available | 2019-05-31T02:17:46Z | - |
dc.date.issued | 2018-09 | - |
dc.identifier.citation | BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v. 39, No. 9, Page. 1083-1089 | en_US |
dc.identifier.issn | 1229-5949 | - |
dc.identifier.uri | https://onlinelibrary.wiley.com/doi/full/10.1002/bkcs.11555 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/106175 | - |
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. | en_US |
dc.description.sponsorship | We are grateful to the US National Institute of Mental Health (NIMH) Psychoactive Drug Screening Program (contract: HHSN-271-2008-00025-C) for providing binding affinity data. This research is supported by the Original Technology Research Program (NRF-2016M3C7A1904344) funded by the National Research Foundation of Korea (NRF). And this work is additionally funded by the Korea Institute of Science and Technology (KIST) (2E27870 and 2E28412). | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | WILEY-V C H VERLAG GMBH | en_US |
dc.subject | 5-HT7 receptor | en_US |
dc.subject | Antagonist | en_US |
dc.subject | N-alkyl-carbazole | en_US |
dc.subject | Serotonin | en_US |
dc.subject | GPCR | en_US |
dc.title | Synthesis of N-Alkyl-Carbazole Derivatives as 5-HT7R Antagonists | en_US |
dc.type | Article | en_US |
dc.relation.no | 9 | - |
dc.relation.volume | 39 | - |
dc.identifier.doi | 10.1002/bkcs.11555 | - |
dc.relation.page | 1083-1089 | - |
dc.relation.journal | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.contributor.googleauthor | Kim, Youngjae | - |
dc.contributor.googleauthor | Yeom, Miyoung | - |
dc.contributor.googleauthor | Lee, Soyeon | - |
dc.contributor.googleauthor | Tae, Jinsung | - |
dc.contributor.googleauthor | Kim, Hak Joong | - |
dc.contributor.googleauthor | Rhim, Hyewhon | - |
dc.contributor.googleauthor | Seong, Jihye | - |
dc.contributor.googleauthor | Choi, Kyung Il | - |
dc.contributor.googleauthor | Min, Sun-Joon | - |
dc.contributor.googleauthor | Choo, Hyunah | - |
dc.relation.code | 2018000145 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY[E] | - |
dc.sector.department | DEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING | - |
dc.identifier.pid | sjmin | - |
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