About: Substituted imidazopyridines as potent inhibitors of HCV replication

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.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	Substituted imidazopyridines as potent inhibitors of HCV replication
Creator	De Burghgraeve, Tine Neyts, Johan De Clercq, Erik Paeshuyse, Jan Boddeker, Nina Bondy, Steven Mabery, Eric Oare, David Paulson, Matthew Pürstinger, Gerhard Reiser, Hans Shih, I-Hung Vliegen, Inge Zhong, Weidong Lee, William Lehman, Laura
Source	Elsevier; Medline; PMC
abstract	Background/Aims Following lead optimization, a set of substituted imidazopyridines was identified as potent and selective inhibitors of in vitro HCV replication. The particular characteristics of one of the most potent compounds in this series (5-[[3-(4-chlorophenyl)-5-isoxazolyl]methyl]-2-(2,3-difluorophenyl)-5H-imidazo[4,5-c]pyridine or GS-327073), were studied. Methods Antiviral activity of GS-327073 was evaluated in HCV subgenomic replicons (genotypes 1b, 1a and 2a), in the JFH1 (genotype 2a) infectious system and against replicons resistant to various selective HCV inhibitors. Combination studies of GS-327073 with other selective HCV inhibitors were performed. Results Fifty percent effective concentrations for inhibition of HCV subgenomic 1b replicon replication ranged between 2 and 50nM and were 100-fold higher for HCV genotype 2a virus. The 50% cytostatic concentrations were ⩾17μM, thus resulting in selectivity indices of ⩾340. GS-327073 retained wild-type activity against HCV replicons that were resistant to either HCV protease inhibitors or several polymerase inhibitors. GS-327073, when combined with either interferon α, ribavirin, a nucleoside polymerase or a protease inhibitor resulted in overall additive antiviral activity. Combinations containing GS-327073 proved highly effective in clearing hepatoma cells from HCV. Conclusions GS-327073 is a potent in vitro inhibitor of HCV replication either alone or in combination with other selective HCV inhibitors.
has issue date	2009-05-31(xsd:dateTime)
bibo:doi	10.1016/j.jhep.2008.12.028
bibo:pmid	19303654
has license	els-covid
sha1sum (hex)	9e5360d3283ac39f7a943482183c90dc00bdfa9d
schema:url	https://doi.org/10.1016/j.jhep.2008.12.028
resource representing a document's title	Substituted imidazopyridines as potent inhibitors of HCV replication
has PubMed Central identifier	PMC7114863
has PubMed identifier	19303654
schema:publication	Journal of Hepatology
resource representing a document's body	covid:9e5360d3283ac39f7a943482183c90dc00bdfa9d#body_text
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