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dc.contributor.author | Mizuhara, Tsukasa | en |
dc.contributor.author | Oishi, Shinya | en |
dc.contributor.author | Ohno, Hiroaki | en |
dc.contributor.author | Shimura, Kazuya | en |
dc.contributor.author | Matsuoka, Masao | en |
dc.contributor.author | Fujii, Nobutaka | en |
dc.contributor.alternative | 大石, 真也 | ja |
dc.date.accessioned | 2012-11-12T00:24:15Z | - |
dc.date.available | 2012-11-12T00:24:15Z | - |
dc.date.issued | 2012-11-01 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/2433/161054 | - |
dc.description.abstract | 3, 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. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier BV | en |
dc.rights | © 2012 Elsevier Ltd. | en |
dc.rights | This is not the published version. Please cite only the published version. | en |
dc.rights | 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.subject | Anti-HIV agents | en |
dc.subject | PD 404182 | en |
dc.subject | Pyrimidobenzothiazine | en |
dc.title | Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents. | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10938083 | - |
dc.identifier.jtitle | Bioorganic & medicinal chemistry | en |
dc.identifier.volume | 20 | - |
dc.identifier.issue | 21 | - |
dc.identifier.spage | 6434 | - |
dc.identifier.epage | 6441 | - |
dc.relation.doi | 10.1016/j.bmc.2012.08.030 | - |
dc.textversion | author | - |
dc.identifier.pmid | 23022280 | - |
dcterms.accessRights | open access | - |
dc.identifier.pissn | 0968-0896 | - |
出現コレクション: | 学術雑誌掲載論文等 |
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