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Title: Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin-6-imine derivatives for potent anti-HIV agents.
Authors: Mizuhara, Tsukasa
Oishi, Shinya  kyouindb  KAKEN_id  orcid (unconfirmed)
Ohno, Hiroaki  kyouindb  KAKEN_id  orcid (unconfirmed)
Shimura, Kazuya  kyouindb  KAKEN_id  orcid (unconfirmed)
Matsuoka, Masao  KAKEN_id
Fujii, Nobutaka  KAKEN_id
Author's alias: 大石, 真也
Keywords: Anti-HIV agents
PD 404182
Issue Date: 1-Nov-2012
Publisher: Elsevier Ltd.
Journal title: Bioorganic & medicinal chemistry
Volume: 20
Issue: 21
Start page: 6434
End page: 6441
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.
Rights: © 2012 Elsevier Ltd.
This 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。
DOI(Published Version): 10.1016/j.bmc.2012.08.030
PubMed ID: 23022280
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