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タイトル: Concise synthesis and anti-HIV activity of pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic heterocycles.
著者: Mizuhara, Tsukasa
Oishi, Shinya  kyouindb  KAKEN_id
Ohno, Hiroaki  kyouindb  KAKEN_id
Shimura, Kazuya  kyouindb  KAKEN_id
Matsuoka, Masao  KAKEN_id
Fujii, Nobutaka  KAKEN_id
著者名の別形: 大石, 真也
発行日: 22-Jun-2012
出版者: Royal Society of Chemistry
誌名: Organic & biomolecular chemistry
巻: 10
号: 33
開始ページ: 6792
終了ページ: 6802
抄録: 3, 4-Dihydro-2H, 6H-pyrimido[1, 2-c][1, 3]benzothiazin-6-imine (PD 404182) is a virucidal heterocyclic compound active against various viruses, including HCV, HIV, and simian immunodeficiency virus. Using facile synthetic approaches that we developed for the synthesis of pyrimido[1, 2-c][1, 3]benzothiazin-6-imines and related tricyclic derivatives, the parallel structural optimizations of the central 1, 3-thiazin-2-imine core, the benzene part, and the cyclic amidine part of PD 404182 were investigated. Replacement of the 6-6-6 pyrimido[1, 2-c][1, 3]benzothiazin-6-imine framework with 5-6-6 or 6-6-5 derivatives led to a significant loss of anti-HIV activity, and introduction of a hydrophobic group at the 9- or 10-positions improved the potency. In addition, we demonstrated that the PD 404182 derivative exerts anti-HIV effects at an early stage of viral infection.
著作権等: © The Royal Society of Chemistry 2012.
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。
URI: http://hdl.handle.net/2433/176376
DOI(出版社版): 10.1039/c2ob25904d
PubMed ID: 22829059
出現コレクション:学術雑誌掲載論文等

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