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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 https://orcid.org/0000-0002-2833-2539 (unconfirmed) Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed) Shimura, Kazuya https://orcid.org/0000-0001-7819-5184 (unconfirmed) Matsuoka, Masao Fujii, Nobutaka |
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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