DSpace at KISTKIST Article2012

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dc.contributor.authorYoo, Euna-
dc.contributor.authorHayat, Faisal-
dc.contributor.authorRhim, Hyewhon-
dc.contributor.authorChoo, Hea-Young Park-
dc.date.accessioned2024-01-20T15:02:17Z-
dc.date.available2024-01-20T15:02:17Z-
dc.date.created2021-09-04-
dc.date.issued2012-04-15-
dc.identifier.issn0968-0896-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/129333-
dc.description.abstractA series of novel N,N-dimethyl-N'-(5-(Ar-sulfonamido) benzo[d]isothiazol-3-yl)formimidamides was designed and synthesized as 5-HT6 ligands. Here N,N-dimethyl formimidamides was used as a replacement for an aminoethyl moiety. In vitro functional assays demonstrated compounds 9b and 9i significantly inhibited the 5-HT-induced Ca2+ increases (9b; IC50 = 0.36 mu M and 9i; IC50 = 0.44 mu M), indicating that 9b and 9i were potent 5-HT6 receptor antagonists. Compounds 9i also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors. (C) 2012 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectRAT-
dc.subjectLOCALIZATION-
dc.subjectCLONING-
dc.subjectAFFINITY-
dc.subjectLIGANDS-
dc.subjectPOTENT-
dc.titleSynthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmc.2012.02.020-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY, v.20, no.8, pp.2707 - 2712-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY-
dc.citation.volume20-
dc.citation.number8-
dc.citation.startPage2707-
dc.citation.endPage2712-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000302767100028-
dc.identifier.scopusid2-s2.0-84859428852-
dc.relation.journalWebOfScienceCategoryBiochemistry & Molecular Biology-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaBiochemistry & Molecular Biology-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusRAT-
dc.subject.keywordPlusLOCALIZATION-
dc.subject.keywordPlusCLONING-
dc.subject.keywordPlusAFFINITY-
dc.subject.keywordPlusLIGANDS-
dc.subject.keywordPlusPOTENT-
dc.subject.keywordAuthor5-HT6 receptor antagonists-
dc.subject.keywordAuthorBenzoisothiazole-
dc.subject.keywordAuthorSulfonamide-
dc.subject.keywordAuthorN,N-dimethylformimidamide-
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