{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,7]],"date-time":"2026-04-07T15:40:37Z","timestamp":1775576437945,"version":"3.50.1"},"reference-count":107,"publisher":"MDPI AG","issue":"4","license":[{"start":{"date-parts":[[2023,2,15]],"date-time":"2023-02-15T00:00:00Z","timestamp":1676419200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Cearense Foundation for Support for Scientific and Technological Development (Funcap)","award":["PS1-0186-00188.01.00\/21"],"award-info":[{"award-number":["PS1-0186-00188.01.00\/21"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>The bacterial species Staphylococcus aureus presents a variety of resistance mechanisms, among which the expression of \u03b2-lactamases and efflux pumps stand out for providing a significant degree of resistance to clinically relevant antibiotics. The 1,8-naphthyridines are nitrogen heterocycles with a broad spectrum of biological activities and, as such, are promising research targets. However, the potential roles of these compounds on bacterial resistance management remain to be better investigated. Therefore, the present study evaluated the antibacterial activity of 1,8-naphthyridine sulfonamides, addressing their ability to act as inhibitors of \u03b2-lactamases and efflux pump (QacA\/B and QacC) against the strains SA-K4414 and SA-K4100 of S. aureus. All substances were prepared at an initial concentration of 1024 \u03bcg\/mL, and their minimum inhibitory concentrations (MIC) were determined by the broth microdilution method. Subsequently, their effects on \u03b2-lactamase- and efflux pump-mediated antibiotic resistance was evaluated from the reduction of the MIC of ethidium bromide (EtBr) and \u03b2-lactam antibiotics, respectively. The 1,8-naphthyridines did not present direct antibacterial activity against the strains SA-K4414 and SA-K4100 of S. aureus. On the other hand, when associated with antibiotics against both strains, the compounds reduced the MIC of EtBr and \u03b2-lactam antibiotics, suggesting that they may act by inhibiting \u03b2-lactamases and efflux pumps such as QacC and QacA\/B. However, further research is required to elucidate the molecular mechanisms underlying these observed effects.<\/jats:p>","DOI":"10.3390\/molecules28041819","type":"journal-article","created":{"date-parts":[[2023,2,15]],"date-time":"2023-02-15T02:01:10Z","timestamp":1676426470000},"page":"1819","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":20,"title":["Efflux Pump (QacA, QacB, and QacC) and \u03b2-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Staphylococcus aureus Strains"],"prefix":"10.3390","volume":"28","author":[{"given":"C\u00edcera Datiane de Morais","family":"Oliveira-Tintino","sequence":"first","affiliation":[{"name":"Laboratory of Microbiology and Molecular Biology, Department of Biological Chemistry, Regional University of Cariri (URCA), Crato 63105-000, CE, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7733-9331","authenticated-orcid":false,"given":"Saulo Relison","family":"Tintino","sequence":"additional","affiliation":[{"name":"Laboratory of Microbiology and Molecular Biology, Department of Biological Chemistry, Regional University of Cariri (URCA), Crato 63105-000, CE, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ana Carolina","family":"Justino de Ara\u00fajo","sequence":"additional","affiliation":[{"name":"Laboratory of Microbiology and Molecular Biology, Department of Biological 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University of Paran\u00e1 (UFPR), Curitiba 81531-990, PR, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sandro Lucio","family":"Mireski","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Regional University of Blumenau (FURB), Itoupava Seca, Blumenau 89030-903, SC, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Michele Caroline","family":"Nasato","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Regional University of Blumenau (FURB), Itoupava Seca, Blumenau 89030-903, SC, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria Isabel Lacowicz","family":"Krautler","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Regional University of Blumenau (FURB), Itoupava Seca, Blumenau 89030-903, SC, 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