Synthesis, characterization and biological evaluation of 1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino-3-methylbutanohydrazide hydrazones

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dc.authorid0000-0002-7734-8553en_US
dc.authorscopusid57195413574en_US
dc.contributor.authorTatar, Esra
dc.contributor.authorKüçükgüzel, İlkay
dc.contributor.authorÖtük, Gülten
dc.contributor.authorBilgin, Merve
dc.contributor.authorDe Clercq, Erik
dc.contributor.authorAndrei, Graciela
dc.contributor.authorSnoeck, Robert
dc.contributor.authorPannecouque, Christophe
dc.contributor.authorKaushik-Basu, Neerja
dc.date.accessioned2021-12-20T12:26:26Z
dc.date.available2021-12-20T12:26:26Z
dc.date.issued2021en_US
dc.departmentFakülteler, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalıen_US
dc.description.abstractNovel 2-aryl-5-non-substituted / methyl-1,3-thiazolidine-4-one derivatives 14-33 carrying L-valine core were synthesized by the reaction of acylhydrazones 4-13 with thioglycolic acid / thiolactic acid. Structures of all synthesized compounds 14-33 were confirmed by IR, H-1-NMR and HR-MS analysis and C-13-NMR were recorded for selected compounds 17, 21, 28 and 30. None of the compounds 14-33 showed activity against HIV-1 (strain IIIB) or HIV-2 (strain ROD) in an MT-4/MTT based assay. Compounds 14-33 were also screened against Feline Corona Virus (FIPV), Feline Herpes Virus, HSV-1(KOS), HSV-1 (TK-KOS ACVr), HSV-2 (G), Vaccinia virus, Vesicular stomatitis virus, Cytomegalovirus, Varicella-Zoster virus, Respiratory syncytial virus, Coxsackie B4 virus, Parainfluenza-3 virus, Reovirus-1, Sindbis virus and Punta Toro virus, but none of them showed antiviral activity at subtoxic concentrations. Anti-HCV NS5B RdRp activity of some selected compounds from the series 14-33 were found to vary between 4.1-27 % at the concentration of 100 mu M. In vitro antibacterial activity evaluation of selected compounds 16-23 and 25-32, against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 29212, Klebsiella pneumoniae ATCC 4352, Bacillus subtilis ATCC 6633, Staphylococcus epidermidis ATCC 12228, MRSA and antifungal activity against Candida albicans ATCC 10231 resulted in the MIC values between 625->5000 mu g/ml.en_US
dc.identifier.citationTatar, E., Küçükgüzel, İ., Ötük, G., Bilgin, M., De Clercq, E., Andrei, G., Snoeck, R., Pannecouque, C., & Kaushik-Basu, N. (2021). Synthesis, characterization and biological evaluation of 1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino-3-methylbutanohydrazide hydrazones. Journal of Research in Pharmacy, 25(4), pp. 507-518. https://doi.org/10.29228/jrp.41en_US
dc.identifier.doi10.29228/jrp.41en_US
dc.identifier.endpage518en_US
dc.identifier.issue4en_US
dc.identifier.scopus2-s2.0-85111994963en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage507en_US
dc.identifier.trdizinid459875
dc.identifier.urihttps://doi.org/10.29228/jrp.41
dc.identifier.urihttps://hdl.handle.net/20.500.13055/98
dc.identifier.volume25en_US
dc.identifier.wosWOS:000678159500016en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakTR-Dizinen_US
dc.indekslendigikaynak.otherESCI - Emerging Sources Citation Indexen_US
dc.institutionauthorBilgin, Merve
dc.language.isoenen_US
dc.publisherMarmara University Pressen_US
dc.relation.ispartofJournal of Research in Pharmacyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subject4-Thiazolidinonesen_US
dc.subjectL-valineen_US
dc.subjectAntibacterial Activityen_US
dc.subjectAnti-HIV Activityen_US
dc.subjectAnti-HCV Activityen_US
dc.titleSynthesis, characterization and biological evaluation of 1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino-3-methylbutanohydrazide hydrazonesen_US
dc.typeArticleen_US
dspace.entity.typePublication

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