{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["15(3)"],"submitter":["Canale V"],"pubmed_abstract":["Multidrug-resistant (MDR) strains of <i>Staphylococcus epidermidis</i> (<i>S. epidermidis</i>), prevalent in hospital environments, contribute to increased morbidity and mortality, especially among newborns, posing a critical concern for neonatal sepsis. In response to the pressing demand for novel antibacterial therapies, we present findings from synthetic chemistry and structure-activity relationship studies focused on arylsulfonamide/arylurea derivatives of aryloxy[1-(thien-2-yl)propyl]piperidines. Through bioisosteric replacement of the sulfonamide fragment with a urea moiety, compound <b>25</b> was identified, demonstrating potent bacteriostatic activity against clinical multidrug-resistant <i>S. epidermidis</i> strains (MIC<sub>50</sub> and MIC<sub>90</sub> = 1.6 and 3.125 μg/mL). Importantly, it showed activity against linezolid-resistant strains and exhibited selectivity over mammalian cells. Compound <b>25</b> displayed antibiofilm-forming properties against clinical <i>S. epidermidis</i> strains and demonstrated the capacity to eliminate existing biofilm layers. Additionally, it induced complete depolarization of the bacterial membrane in clinical <i>S. epidermidis</i> strains. In light of these findings, targeting bacterial cell membranes with compound <b>25</b> emerges as a promising strategy in the fight against multidrug-resistant <i>S. epidermidis</i> strains."],"journal":["ACS medicinal chemistry letters"],"pagination":["369-375"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10945555"],"repository":["biostudies-literature"],"pubmed_title":["Improving Activity of New Arylurea Agents against Multidrug-Resistant and Biofilm-Producing <i>Staphylococcus epidermidis</i>."],"pmcid":["PMC10945555"],"pubmed_authors":["Zajdel P","Skiba-Kurek I","Karczewska E","Ropek M","Pomierny B","Canale V","Klesiewicz K","Papiez M","Piska K","Empel J","Koczurkiewicz-Adamczyk P"],"additional_accession":[]},"is_claimable":false,"name":"Improving Activity of New Arylurea Agents against Multidrug-Resistant and Biofilm-Producing <i>Staphylococcus epidermidis</i>.","description":"Multidrug-resistant (MDR) strains of <i>Staphylococcus epidermidis</i> (<i>S. epidermidis</i>), prevalent in hospital environments, contribute to increased morbidity and mortality, especially among newborns, posing a critical concern for neonatal sepsis. In response to the pressing demand for novel antibacterial therapies, we present findings from synthetic chemistry and structure-activity relationship studies focused on arylsulfonamide/arylurea derivatives of aryloxy[1-(thien-2-yl)propyl]piperidines. Through bioisosteric replacement of the sulfonamide fragment with a urea moiety, compound <b>25</b> was identified, demonstrating potent bacteriostatic activity against clinical multidrug-resistant <i>S. epidermidis</i> strains (MIC<sub>50</sub> and MIC<sub>90</sub> = 1.6 and 3.125 μg/mL). Importantly, it showed activity against linezolid-resistant strains and exhibited selectivity over mammalian cells. Compound <b>25</b> displayed antibiofilm-forming properties against clinical <i>S. epidermidis</i> strains and demonstrated the capacity to eliminate existing biofilm layers. Additionally, it induced complete depolarization of the bacterial membrane in clinical <i>S. epidermidis</i> strains. In light of these findings, targeting bacterial cell membranes with compound <b>25</b> emerges as a promising strategy in the fight against multidrug-resistant <i>S. epidermidis</i> strains.","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Mar","modification":"2025-04-26T12:04:59.753Z","creation":"2025-02-19T03:08:27.335Z"},"accession":"S-EPMC10945555","cross_references":{"pubmed":["38505856"],"doi":["10.1021/acsmedchemlett.3c00536"]}}