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Novel Tetrazole-Based Antimicrobial Agents Targeting Clinical Bacteria Strains: Exploring the Inhibition of Staphylococcus aureus DNA Topoisomerase IV and Gyrase

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cris.lastimport.scopus2024-02-12T20:54:22Z
dc.abstract.enEleven novel imide‐tetrazoles were synthesized. In the initial stage of research, in silico structure‐based pharmacological prediction was conducted. All compounds were screened for an-timicrobial activity using standard and clinical strains. Within the studied group, compounds 1–3 were recognized as leading structures with the most promising results in antimicrobial studies. Minimal inhibitory concentration values for compounds 1, 2, 3 were within the range of 0.8–3.2 μg/mL for standard and clinical Gram‐positive and Gram‐negative bacterial strains, showing in some cases higher activity than the reference Ciprofloxacin. Additionally, all three inhibited the growth of all clinical Staphylococci panels: Staphylococcus aureus (T5592; T5591) and Staphylococcus epidermidis (5253; 4243) with MIC values of 0.8 μg/mL. Selected compounds were examined in topoi-somerase IV decatenation assay and DNA gyrase supercoiling assay, followed by suitable molecular docking studies to explore the possible binding modes. In summary, the presented transition from substrate imide‐thioureas to imide‐tetrazole derivatives resulted in significant increase of an-timicrobial properties. The compounds 1–3 proposed here provide a promising basis for further exploration towards novel antimicrobial drug candidates
dc.affiliationUniwersytet Warszawski
dc.contributor.authorSzulczyk, Daniel
dc.contributor.authorStruga, Marta
dc.contributor.authorWrzosek, Małgorzata
dc.contributor.authorKmiecik, Sebastian
dc.contributor.authorKoliński, Michał
dc.contributor.authorSzymańska-Majchrzak, Jolanta
dc.contributor.authorRoszkowski, Piotr
dc.date.accessioned2024-01-25T13:52:39Z
dc.date.available2024-01-25T13:52:39Z
dc.date.copyright2021-12-29
dc.date.issued2022
dc.description.accesstimeAT_PUBLICATION
dc.description.financePublikacja bezkosztowa
dc.description.number1
dc.description.versionFINAL_PUBLISHED
dc.description.volume23
dc.identifier.doi10.3390/IJMS23010378
dc.identifier.issn1422-0067
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/113969
dc.identifier.weblinkhttps://www.mdpi.com/1422-0067/23/1/378/pdf
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.relation.pages378
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enantimicrobial
dc.subject.enantibacterial
dc.subject.entetrazole
dc.subject.engyrase
dc.subject.entopoisomerase
dc.titleNovel Tetrazole-Based Antimicrobial Agents Targeting Clinical Bacteria Strains: Exploring the Inhibition of Staphylococcus aureus DNA Topoisomerase IV and Gyrase
dc.typeJournalArticle
dspace.entity.typePublication