About: Synthesis and anti-influenza virus activity of 4-oxo- or thioxo-4,5-dihydrofuro[3,4-c]pyridin-3(1H)-ones

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About: Synthesis and anti-influenza virus activity of 4-oxo- or thioxo-4,5-dihydrofuro[3,4-c]pyridin-3(1H)-ones Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Synthesis and anti-influenza virus activity of 4-oxo- or thioxo-4,5-dihydrofuro[3,4-c]pyridin-3(1H)-ones
Creator	Kim, Meehyein Lee, Chong-Kyo Achary, Raghavendra Jung, Young-Sik Kim, Pilho Han, Soo Jang, Ye Kang, Nam Lee, Hye Lee, Hyo
Source	Elsevier; Medline; PMC
abstract	Abstract A target-free approach was applied to discover anti-influenza viral compounds, where influenza infected Madin–Darby canine kidney cells were treated 7500 different small organic chemicals individually and reduction of virus-induced cytopathic effect was measured. One of the hit compounds was (Z)-1-((5-fluoro-1H-indol-3-yl)methylene)-6-methyl-4-thioxo-4,5-dihydrofuro[3,4- c ]pyridin-3(1H)-one (15a) with half-maximal effective concentrations of 17.4–21.1μM against influenza A/H1N1, A/H3N2 and B viruses without any cellular toxicity at 900μM. To investigate the structure–activity relationships, two dozens of the hit analogs were synthesized. Among them, 15g, 15j, 15q, 15s, 15t and 15x had anti-influenza viral activity comparable or superior to that of the initial hit. The anti-influenza viral compounds efficiently suppressed not only viral protein level of the infected cells but also production of viral progeny in the culture supernatants in a dose-dependent manner. Based on a mode-of-action study, they did not affect virus entry or RNA replication. Instead, they suppressed viral neuraminidase activity. This study is the first to demonstrate that dihydrofuropyridinones could serve as lead compounds for the discovery of alternative influenza virus inhibitors.
has issue date	2014-07-31(xsd:dateTime)
bibo:doi	10.1016/j.antiviral.2014.04.013
bibo:pmid	24794525
has license	els-covid
sha1sum (hex)	adbed52aa8470e8fcff48513e6471ac5381e6189
schema:url	https://doi.org/10.1016/j.antiviral.2014.04.013
resource representing a document's title	Synthesis and anti-influenza virus activity of 4-oxo- or thioxo-4,5-dihydrofuro[3,4-c]pyridin-3(1H)-ones
has PubMed Central identifier	PMC7113773
has PubMed identifier	24794525
schema:publication	Antiviral Research
resource representing a document's body	covid:adbed52aa8470e8fcff48513e6471ac5381e6189#body_text
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