{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,16]],"date-time":"2025-12-16T12:44:03Z","timestamp":1765889043112,"version":"build-2065373602"},"reference-count":87,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2023,1,20]],"date-time":"2023-01-20T00:00:00Z","timestamp":1674172800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Antibiotics"],"abstract":"<jats:p>The growing antimicrobial resistance to last-line antimicrobials among Gram-positive pathogens remains a major healthcare emergency worldwide. Therefore, the search for new small molecules targeting multidrug-resistant pathogens remains of great importance. In this paper, we report the synthesis and in vitro antimicrobial activity characterisation of novel thiazole derivatives using representative Gram-negative and Gram-positive strains, including tedizolid\/linezolid-resistant S. aureus, as well as emerging fungal pathogens. The 4-substituted thiazoles 3h, and 3j with naphthoquinone-fused thiazole derivative 7 with excellent activity against methicillin and tedizolid\/linezolid-resistant S. aureus. Moreover, compounds 3h, 3j and 7 showed favourable activity against vancomycin-resistant E. faecium. Compounds 9f and 14f showed broad-spectrum antifungal activity against drug-resistant Candida strains, while ester 8f showed good activity against Candida auris which was greater than fluconazole. Collectively, these data demonstrate that N-2,5-dimethylphenylthioureido acid derivatives could be further explored as novel scaffolds for the development of antimicrobial candidates targeting Gram-positive bacteria and drug-resistant pathogenic fungi.<\/jats:p>","DOI":"10.3390\/antibiotics12020220","type":"journal-article","created":{"date-parts":[[2023,1,20]],"date-time":"2023-01-20T02:43:29Z","timestamp":1674182609000},"page":"220","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and Development of N-2,5-Dimethylphenylthioureido Acid Derivatives as Scaffolds for New Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens"],"prefix":"10.3390","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-3269-8058","authenticated-orcid":false,"given":"Povilas","family":"Kavaliauskas","sequence":"first","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"},{"name":"Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 1300 York Ave., New York, NY 10065, USA"},{"name":"Institute for Genome Sciences, School of Medicine, University of Maryland, 655 W. Baltimore Street, Baltimore, MD 21201, USA"},{"name":"Institute of Infectious Diseases and Pathogenic Microbiology, Bir\u0161tono Str. 38A, LT-59116 Prienai, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Birut\u0117","family":"Grybait\u0117","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rita","family":"Vaickelionien\u0117","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Birut\u0117","family":"Sapijanskait\u0117-Banevi\u010d","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kazimieras","family":"Anusevi\u010dius","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Agn\u0117","family":"Kriau\u010di\u016bnait\u0117","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Gabriel\u0117","family":"Smailien\u0117","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6811-4467","authenticated-orcid":false,"given":"Vidmantas","family":"Petraitis","sequence":"additional","affiliation":[{"name":"Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 1300 York Ave., New York, NY 10065, USA"},{"name":"Institute of Infectious Diseases and Pathogenic Microbiology, Bir\u0161tono Str. 38A, LT-59116 Prienai, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"R\u016bta","family":"Petraitien\u0117","sequence":"additional","affiliation":[{"name":"Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 1300 York Ave., New York, NY 10065, USA"},{"name":"Institute of Infectious Diseases and Pathogenic Microbiology, Bir\u0161tono Str. 38A, LT-59116 Prienai, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ethan","family":"Naing","sequence":"additional","affiliation":[{"name":"Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 1300 York Ave., New York, NY 10065, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andrew","family":"Garcia","sequence":"additional","affiliation":[{"name":"Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 1300 York Ave., New York, NY 10065, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9961-2941","authenticated-orcid":false,"given":"Vytautas","family":"Mickevi\u010dius","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2023,1,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"e0116821","DOI":"10.1128\/AAC.01168-21","article-title":"Pharmacokinetics, Tissue Distribution, and Efficacy of VIO-001 (Meropenem\/Piperacillin\/Tazobactam) for Treatment of Methicillin-Resistant Staphylococcus Aureus Bacteremia in Immunocompetent Rabbits with Chronic Indwelling Vascular Catheters","volume":"65","author":"Petraitis","year":"2021","journal-title":"Antimicrob. 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