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dc.contributor.authorJang, Jae Wan-
dc.contributor.authorBaek, Je-sook-
dc.contributor.authorChoi, Gil Don-
dc.contributor.authorPark, Woo-Kyu-
dc.contributor.authorCho, Yong Seo-
dc.contributor.authorBaek, Du-Jong-
dc.contributor.authorPae, Ae Nim-
dc.date.accessioned2024-01-20T15:33:36Z-
dc.date.available2024-01-20T15:33:36Z-
dc.date.created2021-09-04-
dc.date.issued2012-01-01-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/129655-
dc.description.abstractAgonists 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.languageEnglish-
dc.publisherPergamon Press Ltd.-
dc.subjectBINDING-
dc.subject5-HYDROXYTRYPTAMINE(2A)-
dc.subjectPACKING-
dc.subjectENERGY-
dc.subjectMICE-
dc.title5-HT2C receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2011.11.001-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, v.22, no.1, pp.347 - 352-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.volume22-
dc.citation.number1-
dc.citation.startPage347-
dc.citation.endPage352-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000298636700066-
dc.identifier.scopusid2-s2.0-84655167900-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusBINDING-
dc.subject.keywordPlus5-HYDROXYTRYPTAMINE(2A)-
dc.subject.keywordPlusPACKING-
dc.subject.keywordPlusENERGY-
dc.subject.keywordPlusMICE-
dc.subject.keywordAuthor5-HT2c ligands-
dc.subject.keywordAuthorObesity-
dc.subject.keywordAuthorSelectivity-
dc.subject.keywordAuthorHomology-
dc.subject.keywordAuthormodeling-
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