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Design and synthesis of novel 1H-tetrazol-5-amine based potent antimicrobial agents: DNA topoisomerase IV and gyrase affinity evaluation supported by molecular docking studies

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dc.abstract.enA total of 14 of 1,5-disubstituted tetrazole derivatives were prepared by reacting appropriate thiourea and sodium azide in the presence of mercury (II) chloride and triethylamine. All compounds were evaluated in vitro for their antimicrobial activity. Derivatives 10 and 11 showed the highest inhibition against Gram-positive and Gram-negative strains (standard and hospital strains). The observed minimal inhibitory concentrations values were in the range of 1–208 μM (0.25–64 μg/ml). Inhibitory activity of 1,5-tetrazole derivatives 10 and 11 against gyrase and topoisomerase IV isolated from S. aureus was studied. Evaluation was supported by molecular docking studies for all synthesized derivatives and reference ciprofloxacin. Moreover, selected tetrazoles (2, 3, 5, 6, 8, 9, 10 and 11) were evaluated for their cytotoxicity. All tested compounds are non-cytotoxic against HaCaT and A549 cells (CC50 ≤ 60 μM).
dc.affiliationUniwersytet Warszawski
dc.contributor.authorDobrowolski, Michał
dc.contributor.authorStefańska, Joanna
dc.contributor.authorSzulczyk, Daniel
dc.contributor.authorOlejarz, Wioletta
dc.contributor.authorKoliński, Michał
dc.contributor.authorKmiecik, Sebastian
dc.contributor.authorStruga, Marta
dc.contributor.authorBielenica, Anna
dc.contributor.authorJóźwiak, Michał
dc.contributor.authorRoszkowski, Piotr
dc.contributor.authorWrzosek, Małgorzata
dc.date.accessioned2024-01-24T21:33:27Z
dc.date.available2024-01-24T21:33:27Z
dc.date.issued2018
dc.description.financeNie dotyczy
dc.description.volume156
dc.identifier.doi10.1016/J.EJMECH.2018.07.041
dc.identifier.issn0223-5234
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/104600
dc.identifier.weblinkhttp://www.sciencedirect.com/
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.pages631-640
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.subject.en1H-tetrazol-5-amine
dc.subject.enAntimicrobial activity
dc.subject.enTopoisomerase type IV
dc.subject.enDNA gyrase
dc.subject.enCytotoxicity
dc.subject.enMolecular docking
dc.titleDesign and synthesis of novel 1H-tetrazol-5-amine based potent antimicrobial agents: DNA topoisomerase IV and gyrase affinity evaluation supported by molecular docking studies
dc.typeJournalArticle
dspace.entity.typePublication