The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Stachyflin and Acetylstachyflin, Novel Anti-influenza A Virus Substances, Produced by Stachybotrys sp. RF-7260
II. Synthesis and Preliminary Structure-Activity Relationships of Stachyflin Derivatives
KAZUYUKI MINAGAWASHUICHI KOUZUKITOSHIYUKI KAMIGAUCHI
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JOURNAL FREE ACCESS

2002 Volume 55 Issue 2 Pages 165-171

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Abstract

Stachyflin and acetylstachyflin, produced by Stachybotrys sp. RF-7260, were found to have potent anti-influenza A virus activity. Stachyflin is a new class of hemagglutinin fusion inhibitors of influenza A virus. Several derivatives were synthesized from acetylstachyflin and subjected to preliminary examination of their structure-activity relationships. Among them, the 3-oxo and 3, 8'-dioxo derivatives showed potent antiviral activity similar to stachyflin. The 3-epi derivative was four times less active than stachyflin. Modification of the 6'-hydroxy group and the C-5' position markedly diminished the antiviral activity.

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© Japan Antibiotics Research Association
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