Full metadata record
DC Field | Value | Language |
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dc.contributor.author | Jang, Jae Wan | - |
dc.contributor.author | Baek, Je-sook | - |
dc.contributor.author | Choi, Gil Don | - |
dc.contributor.author | Park, Woo-Kyu | - |
dc.contributor.author | Cho, Yong Seo | - |
dc.contributor.author | Baek, Du-Jong | - |
dc.contributor.author | Pae, Ae Nim | - |
dc.date.accessioned | 2024-01-20T15:33:36Z | - |
dc.date.available | 2024-01-20T15:33:36Z | - |
dc.date.created | 2021-09-04 | - |
dc.date.issued | 2012-01-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://pubs.kist.re.kr/handle/201004/129655 | - |
dc.description.abstract | Agonists of the 5-HT2C receptor have attracted much attention as therapeutic agents for the treatment of obesity. Subtype selectivity against other 5-HT2 receptors is one of the most important prerequisites for reducing side effects. We present the synthesis of N-methyl-N-(1-methylpiperidin-4-yl) benzenesulfonamide analogs and their structure-activity relationship studies on 5-HT2A and 5-HT2C receptors. Although the compounds showed nanomolar activity to the 5-HT2C receptor, their selectivity against the 5-HT2A receptor was modest to low. Molecular modeling studies using homology modeling and docking simulation revealed that selectivity originated from subtype specific residues. The observed binding modes and receptor-ligand interactions provided us a clue for optimizing the selectivity against the 5-HT2A receptor. (C) 2011 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.publisher | Pergamon Press Ltd. | - |
dc.subject | BINDING | - |
dc.subject | 5-HYDROXYTRYPTAMINE(2A) | - |
dc.subject | PACKING | - |
dc.subject | ENERGY | - |
dc.subject | MICE | - |
dc.title | 5-HT2C receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.bmcl.2011.11.001 | - |
dc.description.journalClass | 1 | - |
dc.identifier.bibliographicCitation | Bioorganic & Medicinal Chemistry Letters, v.22, no.1, pp.347 - 352 | - |
dc.citation.title | Bioorganic & Medicinal Chemistry Letters | - |
dc.citation.volume | 22 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 347 | - |
dc.citation.endPage | 352 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.identifier.wosid | 000298636700066 | - |
dc.identifier.scopusid | 2-s2.0-84655167900 | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.type.docType | Article | - |
dc.subject.keywordPlus | BINDING | - |
dc.subject.keywordPlus | 5-HYDROXYTRYPTAMINE(2A) | - |
dc.subject.keywordPlus | PACKING | - |
dc.subject.keywordPlus | ENERGY | - |
dc.subject.keywordPlus | MICE | - |
dc.subject.keywordAuthor | 5-HT2c ligands | - |
dc.subject.keywordAuthor | Obesity | - |
dc.subject.keywordAuthor | Selectivity | - |
dc.subject.keywordAuthor | Homology | - |
dc.subject.keywordAuthor | modeling | - |
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