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タイトル: | Identification of anti-HIV agents with a novel benzo[4,5]isothiazolo[2,3-a]pyrimidine scaffold. |
著者: | Okazaki, Shiho Mizuhara, Tsukasa Shimura, Kazuya https://orcid.org/0000-0001-7819-5184 (unconfirmed) Murayama, Hiroto Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed) Oishi, Shinya https://orcid.org/0000-0002-2833-2539 (unconfirmed) Matsuoka, Masao Fujii, Nobutaka |
著者名の別形: | 大石, 真也 |
キーワード: | Anti-HIV agent Isothiazolopyrimidine PD 404182 Pyrimidobenzothiazine |
発行日: | 1-Apr-2015 |
出版者: | Elsevier BV |
誌名: | Bioorganic & medicinal chemistry |
巻: | 23 |
号: | 7 |
開始ページ: | 1447 |
終了ページ: | 1452 |
抄録: | 3, 4-Dihydro-2H-benzo[4, 5]isothiazolo[2, 3-a]pyrimidine is a newly identified antiviral agent against human immunodeficiency virus type 1 (HIV-1) infection, derived from 3, 4-dihydro-2H, 6H-pyrimido[1, 2-c][1, 3]benzothiazin-6-imine (PD 404182). The introduction of the hydrophobic 8-aryl substituent on the benzene substructure improved its anti-HIV activity, resulting in the identification of 6-fold more potent analogs. In addition, it was demonstrated that these isothiazolopyrimidine derivatives exert anti-HIV effects at an early stage of viral infection. |
著作権等: | © 2015. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ The full-text file will be made open to the public on 1 April 2017 in accordance with publisher's 'Terms and Conditions for Self-Archiving' 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。 This is not the published version. Please cite only the published version. |
URI: | http://hdl.handle.net/2433/200802 |
DOI(出版社版): | 10.1016/j.bmc.2015.02.015 |
PubMed ID: | 25744188 |
出現コレクション: | 学術雑誌掲載論文等 |
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