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Title: Identification of anti-HIV agents with a novel benzo[4,5]isothiazolo[2,3-a]pyrimidine scaffold.
Authors: Okazaki, Shiho
Mizuhara, Tsukasa
Shimura, Kazuya  kyouindb  KAKEN_id  orcid (unconfirmed)
Murayama, Hiroto
Ohno, Hiroaki  kyouindb  KAKEN_id  orcid (unconfirmed)
Oishi, Shinya  kyouindb  KAKEN_id  orcid (unconfirmed)
Matsuoka, Masao
Fujii, Nobutaka
Author's alias: 大石, 真也
Keywords: Anti-HIV agent
PD 404182
Issue Date: 1-Apr-2015
Publisher: Elsevier Ltd.
Journal title: Bioorganic & medicinal chemistry
Volume: 23
Issue: 7
Start page: 1447
End page: 1452
Abstract: 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.
Rights: © 2015. This manuscript version is made available under the CC-BY-NC-ND 4.0 license
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'
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.2015.02.015
PubMed ID: 25744188
Appears in Collections:Journal Articles

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