Title Synthesis of 3-((4-hydroxyphenyl)amino)propanoic acid derivatives as promising scaffolds for the development of antimicrobial candidates targeting multidrug-resistant bacterial and fungal pathogens /
Authors Kavaliauskas, Povilas ; Grybaitė, Birutė ; Sapijanskaitė-Banevič, Birutė ; Vaickelionienė, Rita ; Petraitis, Vidmantas ; Petraitienė, Rūta ; Naing, Ethan ; Garcia, Andrew ; Grigalevičiūtė, Ramunė ; Mickevičius, Vytautas
DOI 10.3390/antibiotics13020193
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Is Part of Antibiotics.. Basel : MDPI. 2024, vol. 13, iss. 2, art. no. 193, p. 1-24.. ISSN 2079-6382
Keywords [eng] ESKAPE group pathogens ; amino acid derivatives ; 4-hydroxyphenyl moiety
Abstract [eng] Infections caused by multidrug-resistant bacterial and fungal pathogens represent a significant global health concern, contributing to increased morbidity and mortality rates. Therefore, it is crucial to develop novel compounds targeting drug-resistant microbial strains. Herein, we report the synthesis of amino acid derivatives bearing an incorporated 4-hydroxyphenyl moiety with various substitutions. The resultant novel 3-((4-hydroxyphenyl)amino)propanoic acid derivatives 2–37 exhibited structure-dependent antimicrobial activity against both ESKAPE group bacteria and drug-resistant Candida species. Furthermore, these derivatives demonstrated substantial activity against Candida auris, with minimum inhibitory concentrations ranging from 0.5 to 64 µg/mL. Hydrazones 14–16, containing heterocyclic substituents, showed the most potent and broad-spectrum antimicrobial activity. This activity extended to methicillin-resistant Staphylococcus aureus (MRSA) with MIC values ranging from 1 to 8 µg/mL, vancomycin-resistant Enterococcus faecalis (0.5–2 µg/mL), Gram-negative pathogens (MIC 8–64 µg/mL), and drug-resistant Candida species (MIC 8–64 µg/mL), including Candida auris. Collectively, these findings underscore the potential utility of the novel 3-((4-hydroxyphenyl)amino)propanoic acid scaffold for further development as a foundational platform for novel antimicrobial agents targeting emerging and drug-resistant bacterial and fungal pathogens.
Published Basel : MDPI
Type Journal article
Language English
Publication date 2024
CC license CC license description