Synthesis and evaluation of di-heterocyclic benzazole compounds as potential antibacterial and anti-biofilm agents against Staphylococcus aureus

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dc.contributor.authorAktekin, Mine Buga
dc.contributor.authorOksuz, Zehra
dc.contributor.authorTurkmenoglu, Burcin
dc.contributor.authorIstifli, Erman Salih
dc.contributor.authorKuzucu, Mehmet
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2025-03-17T12:25:37Z
dc.date.available2025-03-17T12:25:37Z
dc.date.issued2024
dc.departmentTarsus Üniversitesi
dc.description.abstractCumulative escalation in antibiotic-resistant pathogens necessitates the quest for novel antimicrobial agents, as current options continue to diminish bacterial resistance. Herein, we report the synthesis of di-heterocyclic benzazole structures (12-19) and their in vitro evaluation for some biological activities. Compounds 16 and 17 demonstrated potent antibacterial activity (MIC = 7.81 mu g/mL) against Staphylococcus aureus, along with significant anti-biofilm activity. Noteworthy is the capability of Compound 17 to inhibit biofilm formation by at least 50% at sub-MIC (3.90 mu g/mL) concentration. Furthermore, both compounds exhibited the potential to inhibit preformed biofilm by at least 50% at the MIC concentration (7.81 mu g/mL). Additionally, Compounds 16 and 17 were examined for cytotoxic effects in HFF-1 cells, using the MTT method, and screened for binding interactions within the active site of S. aureus DNA gyrase using in silico molecular docking technique, employing AutoDock 4.2.6 and Schr & ouml;dinger Glidse programs. Overall, our findings highlight Compounds 16 and 17 as promising scaffolds warranting further optimization for the development of effective antibacterial and anti-biofilm agents.
dc.description.sponsorshipMersin University [2021-1-TP3-4120]
dc.description.sponsorshipMersin University, Grant/Award Number: 2021-1-TP3-4120
dc.identifier.doi10.1111/cbdd.14601
dc.identifier.issn1747-0277
dc.identifier.issn1747-0285
dc.identifier.issue2
dc.identifier.pmid39085984
dc.identifier.scopus2-s2.0-85200154626
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1111/cbdd.14601
dc.identifier.urihttps://hdl.handle.net/20.500.13099/1783
dc.identifier.volume104
dc.identifier.wosWOS:001281451200001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofChemical Biology & Drug Design
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.snmzKA_WOS_20250316
dc.subjectanti-biofilm activity
dc.subjectantimicrobial
dc.subjectcytotoxicity
dc.subjectdi-heterocyclic benzazole
dc.subjectmolecular docking
dc.subjectsynthesis
dc.titleSynthesis and evaluation of di-heterocyclic benzazole compounds as potential antibacterial and anti-biofilm agents against Staphylococcus aureus
dc.typeArticle

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