Title Synthesis and development of N-2,5-dimethylphenylthioureido acid derivatives as scaffolds for new antimicrobial candidates targeting multidrug-resistant gram-positive pathogens /
Authors Kavaliauskas, Povilas ; Grybaitė, Birutė ; Vaickelionienė, Rita ; Sapijanskaitė-Banevič, Birutė ; Anusevičius, Kazimieras ; Kriaučiūnaitė, Agnė ; Smailienė, Gabrielė ; Petraitis, Vidmantas ; Petraitienė, Rūta ; Naing, Ethan ; Garcia, Andrew ; Mickevičius, Vytautas
DOI 10.3390/antibiotics12020220
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Is Part of Antibiotics.. Basel : MDPI. 2023, vol. 12, iss. 2, art. no. 220, p. 1-27.. ISSN 2079-6382
Keywords [eng] 2-aminothiazoles ; antifungal ; antibacterial ; anticancer activity ; hydrazone ; benzimidazole ; sulphanilamide
Abstract [eng] 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.
Published Basel : MDPI
Type Journal article
Language English
Publication date 2023
CC license CC license description