Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 민선준 | - |
dc.date.accessioned | 2018-06-28T07:31:33Z | - |
dc.date.available | 2018-06-28T07:31:33Z | - |
dc.date.issued | 2017-08 | - |
dc.identifier.citation | MOLECULES, v. 22, No. 9, Article no. 1416 | en_US |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | http://www.mdpi.com/1420-3049/22/9/1416/htm | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/72263 | - |
dc.description.abstract | A series of pyrimidine derivatives 4a-i were synthesized and evaluated for their binding affinities towards 5-HT2C receptors. With regard to designed molecules 4a-i, the influence of the size of alkyl ether and the absolute configuration of a stereogenic center on the 5-HT2C binding affinity and selectivity was studied. The most promising diasteromeric mixtures 4d and 4e were selected in the initial radioligand binding assay and they were further synthesized as optically active forms starting from optically active alcohols 5d and 5e, prepared by an enzymatic kinetic resolution. Pyrimidine analogue (R,R)-4e displayed an excellent 5-HT2C binding affinity with good selectivity values against a broad range of other 5-HT receptor subtypes. | en_US |
dc.description.sponsorship | This work was financially supported by the Korea Health Industry Development Institute (KHIDI, HI16C1677, HI17C1037) and the National Research Foundation (NRF-2016R1A2B1012277). Binding affinity data were generously provided by the US National Institute of Mental Health (NIMH) Psychoactive Drug Screening Program (HHSN-271-2008-00025-C). | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | MDPI AG | en_US |
dc.subject | pyrimidine | en_US |
dc.subject | optically active | en_US |
dc.subject | enzymatic kinetic resolution | en_US |
dc.subject | 5-HT2C receptor | en_US |
dc.subject | binding affinity | en_US |
dc.subject | selectivity | en_US |
dc.title | Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators | en_US |
dc.type | Article | en_US |
dc.relation.no | 9 | - |
dc.relation.volume | 22 | - |
dc.identifier.doi | 10.3390/molecules22091416 | - |
dc.relation.page | 1-17 | - |
dc.relation.journal | MOLECULES | - |
dc.contributor.googleauthor | Kim, Juhyeon | - |
dc.contributor.googleauthor | Jo, Hanbyeol | - |
dc.contributor.googleauthor | Lee, Hyunseung | - |
dc.contributor.googleauthor | Choo, Hyunah | - |
dc.contributor.googleauthor | Kim, Hak Joong | - |
dc.contributor.googleauthor | Pae, Ae Nim | - |
dc.contributor.googleauthor | Cho, Yong Seo | - |
dc.contributor.googleauthor | Min, Sun-Joon | - |
dc.relation.code | 2017007269 | - |
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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