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2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase

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dc.contributor.authorTATAR, ESRA
dc.contributor.authorsKucukguzel, Ilkay; Satilmis, Gokhan; Gurukumar, K. R.; Basu, Amartya; Tatar, Esra; Nichols, Daniel B.; Talele, Tanaji T.; Kaushik-Basu, Neerja
dc.date.accessioned2022-03-14T10:54:59Z
dc.date.available2022-03-14T10:54:59Z
dc.date.issued2013-11
dc.description.abstractHepatitis C virus (HCV) NS5B polymerase is an important and attractive target for the development of anti-HCV drugs. Here we report on the design, synthesis and evaluation of twenty-four novel allosteric inhibitors bearing the 4-thiazolidinone scaffold as inhibitors of HCV NS5B polymerase. Eleven compounds tested were found to inhibit HCV NS5B with IC50 values ranging between 19.8 and 64.9 RM. Compound 24 was the most active of this series with an IC50 of 5.6 mu M. A number of these derivatives further exhibited strong inhibition against HCV lb and 2a genotypes in cell based antiviral assays. Molecular docking analysis predicted that the thiazolidinone derivatives bind to the NS5B thumb pocketII (TP-II). Our results suggest that further optimization of the thiazolidinone scaffold may be possible to yield new derivatives with improved enzyme- and cell-based activity. (C) 2013 Elsevier Masson SAS. All rights reserved.
dc.identifier.doi10.1016/j.ejmech.2013.08.043
dc.identifier.eissn1768-3254
dc.identifier.issn0223-5234
dc.identifier.pubmed24161679
dc.identifier.urihttps://hdl.handle.net/11424/245453
dc.identifier.wosWOS:000330603900088
dc.language.isoeng
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
dc.relation.ispartofEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAntiviral agents
dc.subjectHepatitis C
dc.subjectHCV NS5B polymerase
dc.subjectThiazolidinones
dc.subjectDEPENDENT RNA-POLYMERASE
dc.subjectC VIRUS-INFECTION
dc.subjectANTIMICROBIAL ACTIVITY
dc.subjectCRYSTAL-STRUCTURE
dc.subjectIN-VITRO
dc.subjectBIOLOGICAL EVALUATION
dc.subjectHEPATITIS
dc.subject4-THIAZOLIDINONES
dc.subjectDERIVATIVES
dc.subjectDESIGN
dc.title2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase
dc.typearticle
dspace.entity.typePublication
local.avesis.idff4e5cd3-ea89-4105-b3a5-eb242a0f3165
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.numberofpages11
oaire.citation.endPage941
oaire.citation.startPage931
oaire.citation.titleEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
oaire.citation.volume69
relation.isAuthorOfPublicatione2c939bf-1387-4174-802c-e714419b20af
relation.isAuthorOfPublication.latestForDiscoverye2c939bf-1387-4174-802c-e714419b20af

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