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oai:ebyu-rdlopen.rawdatalibrary.net:ebyu/110402026-10-18T21:13:16Zopenairedrivercom_ebyu_10000col_ebyu_10001

Synthesis and evaluation of di-heterocyclic benzazole compounds as potential antibacterial and anti-biofilm agents against Staphylococcus aureusAktekin, Mine BugaOksuz, ZehraTurkmenoglu, BurcinIstifli, Erman SalihKuzucu, MehmetAlgul, Oztekinanti-biofilm activityantimicrobialcytotoxicitydi-heterocyclic benzazolemolecular dockingsynthesis2 mercaptobenzothiazole2 [[(5 chloro 1h benzo[d]imidazol 2 yl)methyl]thio]benzo[d]oxazole2 [[(5 chloro 1h benzo[d]imidazol 2 yl)methyl]thio]benzo[d]thiazolealcoholampicillinaniline derivativeantibiotic agentbenzimidazole derivativechloroacetic acidDNA topoisomerase (ATP hydrolysing)methotrexatepotassium hydroxideunclassified drugwaterantibacterial activityantibiofilm activityantimicrobial activityArticlebinding affinitybiofilmcarbon nuclear magnetic resonancecomputer modelcontrolled studycytotoxicity assayCumulative 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 μg/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 μg/mL) concentration. Furthermore, both compounds exhibited the potential to inhibit preformed biofilm by at least 50% at the MIC concentration (7.81 μg/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 Schrödinger 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. © 2024 The Author(s). Chemical Biology & Drug Design published by John Wiley & Sons Ltd.John Wiley and Sons Inc2024Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/11040https://doi.org/10.1111/cbdd.146011747-0277enChemical Biology and Drug Designinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/11040