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dc.contributor.authorHayat, Faisal-
dc.contributor.authorViswanath, Ambily Nath Indu-
dc.contributor.authorPae, Ae Nim-
dc.contributor.authorRhim, Hyewhon-
dc.contributor.authorPark, Woo-Kyu-
dc.contributor.authorChoo, Hea-Young Park-
dc.date.accessioned2024-01-20T07:32:13Z-
dc.date.available2024-01-20T07:32:13Z-
dc.date.created2021-09-05-
dc.date.issued2015-03-15-
dc.identifier.issn0968-0896-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/125662-
dc.description.abstractA novel series of 4-nitroindole sulfonamides containing a methyleneamino-N,N-dimethylformamidine were prepared. The binding of these compounds to 5-HT2A and 5-HT2C was evaluated, and most of the compounds showed IC50 values of less than 1 mu M, and exhibited high selectivity for the 5-HT2C receptor. However, little selectivity was observed in the functional assay for 5-HT6 receptors. The computational modeling studies further validated the biological results and also demonstrated a reasonable correlation between the activity of compounds and the mode of superimposition with specified pharmacophoric features. (C) 2015 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectCYS23SER POLYMORPHISM-
dc.subjectSEROTONIN-
dc.subjectLIGANDS-
dc.subjectBINDING-
dc.subjectRAT-
dc.titleSynthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmc.2015.01.032-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBIOORGANIC & MEDICINAL CHEMISTRY, v.23, no.6, pp.1313 - 1320-
dc.citation.titleBIOORGANIC & MEDICINAL CHEMISTRY-
dc.citation.volume23-
dc.citation.number6-
dc.citation.startPage1313-
dc.citation.endPage1320-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000349967600010-
dc.identifier.scopusid2-s2.0-84923534690-
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.keywordPlusCYS23SER POLYMORPHISM-
dc.subject.keywordPlusSEROTONIN-
dc.subject.keywordPlusLIGANDS-
dc.subject.keywordPlusBINDING-
dc.subject.keywordPlusRAT-
dc.subject.keywordAuthor4-Nitroindole-
dc.subject.keywordAuthorSulfonamides-
dc.subject.keywordAuthorMethyleneamino-N,N-dimethylformamidine group-
dc.subject.keywordAuthor5-HT2A-
dc.subject.keywordAuthor5-HT2C-
dc.subject.keywordAuthor5-HT6 receptor-
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