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dc.contributor.authorMizuhara, Tsukasaja
dc.contributor.authorOishi, Shinyaja
dc.contributor.authorOhno, Hiroakija
dc.contributor.authorShimura, Kazuyaja
dc.contributor.authorMatsuoka, Masaoja
dc.contributor.authorFujii, Nobutakaja
dc.contributor.alternative大石, 真也ja
dc.date.accessioned2012-11-12T00:24:15Z-
dc.date.available2012-11-12T00:24:15Z-
dc.date.issued2012-11-01ja
dc.identifier.issn0968-0896ja
dc.identifier.urihttp://hdl.handle.net/2433/161054-
dc.description.abstract3, 4-Dihydro-2H, 6H-pyrimido[1, 2-c][1, 3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimido[1, 2-c][1, 3]benzothiazin-6-imine were investigated for the development of more potent anti-HIV agents. Several different derivatives containing a 9-aryl group were designed and synthesized using Suzuki-Miyaura cross-coupling and Ullmann coupling reactions. Modification of the m-methoxyphenyl or benzo[d][1, 3]dioxol-5-yl group resulted in improved anti-HIV activity. In addition, the 2, 4-diazaspiro[5.5]undec-2-ene-fused benzo[e][1, 3]thiazine derivatives were designed and tested for their anti-HIV activities. The most potent 9-(benzo[d][1, 3]dioxol-5-yl) derivative was two-threefold more effective against several strains of HIV-1 and HIV-2 than the parent compound, PD 404182.ja
dc.format.mimetypeapplication/pdfja
dc.language.isoengja
dc.publisherElsevier Ltd.ja
dc.rights© 2012 Elsevier Ltd.ja
dc.rightsThis is not the published version. Please cite only the published version. この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。ja
dc.subjectAnti-HIV agentsja
dc.subjectPD 404182ja
dc.subjectPyrimidobenzothiazineja
dc.titleStructure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents.ja
dc.type.niitypeJournal Articleja
dc.identifier.ncidAA11522681ja
dc.identifier.jtitleBioorganic & medicinal chemistryja
dc.identifier.volume20ja
dc.identifier.issue21ja
dc.identifier.spage6434ja
dc.identifier.epage6441ja
dc.relation.doi10.1016/j.bmc.2012.08.030ja
dc.textversionauthorja
dc.identifier.pmid23022280ja
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