{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,29]],"date-time":"2026-09-29T19:12:47Z","timestamp":1790709167175,"version":"4.1.0"},"reference-count":75,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2021,12,23]],"date-time":"2021-12-23T00:00:00Z","timestamp":1640217600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Rapidly growing antimicrobial resistance among clinically important bacterial and fungal pathogens accounts for high morbidity and mortality worldwide. Therefore, it is critical to look for new small molecules targeting multidrug-resistant pathogens. Herein, in this paper we report a synthesis, ADME properties, and in vitro antimicrobial activity characterization of novel thiazole derivatives bearing \u03b2-amino acid, azole, and aromatic moieties. The in silico ADME characterization revealed that compounds 1\u20139 meet at least 2 Lipinski drug-like properties while cytotoxicity studies demonstrated low cytotoxicity to Vero cells. Further in vitro antimicrobial activity characterization showed the selective and potent bactericidal activity of 2a\u2013c against Gram-positive pathogens (MIC 1\u201364 \u00b5g\/mL) with profound activity against S. aureus (MIC 1\u20132 \u00b5g\/mL) harboring genetically defined resistance mechanisms. Furthermore, the compounds 2a\u2013c exhibited antifungal activity against azole resistant A. fumigatus, while only 2b and 5a showed antifungal activity against multidrug resistant yeasts including Candida auris. Collectively, these results demonstrate that thiazole derivatives 2a\u2013c and 5a could be further explored as a promising scaffold for future development of antifungal and antibacterial agents targeting highly resistant pathogenic microorganisms.<\/jats:p>","DOI":"10.3390\/molecules27010074","type":"journal-article","created":{"date-parts":[[2021,12,23]],"date-time":"2021-12-23T21:40:21Z","timestamp":1640295621000},"page":"74","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":23,"title":["Synthesis of Novel Thiazole Derivatives Bearing \u03b2-Amino Acid and Aromatic Moieties as Promising Scaffolds for the Development of New Antibacterial and Antifungal Candidates Targeting Multidrug-Resistant Pathogens"],"prefix":"10.3390","volume":"27","author":[{"given":"Dovil\u0117","family":"Mal\u016bkait\u0117","sequence":"first","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"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":[{"vocabulary":"crossref","role":"author"}]},{"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":[{"vocabulary":"crossref","role":"author"}]},{"given":"Giedrius","family":"Vaickelionis","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"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":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0237-9088","authenticated-orcid":false,"given":"Povilas","family":"Kavaliauskas","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Kaunas University of Technology, Radvil\u0117n\u0173 Rd. 19, LT-50254 Kaunas, Lithuania"},{"name":"Weill Cornell Medicine of Cornell University, 527 East 68th Street, 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":"Biological Research Center, Veterinary Academy, Lithuanian University of Health Sciences, Til\u017e\u0117s Str. 18, LT-47181 Kaunas, Lithuania"},{"name":"Institute of Infectious Diseases and Pathogenic Microbiology, Bir\u0161tono Str. 38A, LT-59116 Prienai, Lithuania"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"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":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2021,12,23]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"140","DOI":"10.3389\/fpubh.2020.00140","article-title":"Antimicrobial Stewardship Programs in Resource Constrained Environments: Understanding and Addressing the Need of the Systems","volume":"8","author":"Kakkar","year":"2020","journal-title":"Front. 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