Cover Image

Synthesis and Development of <i>N</i>-2,5-Dimethylphenylthioureido Acid Derivatives as Scaffolds for New Antimicrobial Candidates Targeting Multidrug-Resistant Gram-Positive Pathogens

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...

Full description

Saved in:
Bibliographic Details
Main Authors: Povilas Kavaliauskas (Author), Birutė Grybaitė (Author), Rita Vaickelionienė (Author), Birutė Sapijanskaitė-Banevič (Author), Kazimieras Anusevičius (Author), Agnė Kriaučiūnaitė (Author), Gabrielė Smailienė (Author), Vidmantas Petraitis (Author), Rūta Petraitienė (Author), Ethan Naing (Author), Andrew Garcia (Author), Vytautas Mickevičius (Author)
Format: Book
Published: MDPI AG, 2023-01-01T00:00:00Z.
Subjects:
article
Online Access:Connect to this object online.
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 <i>S. aureus,</i> as well as emerging fungal pathogens. The 4-substituted thiazoles <b>3h</b>, and <b>3j</b> with naphthoquinone-fused thiazole derivative <b>7</b> with excellent activity against methicillin and tedizolid/linezolid-resistant <i>S. aureus</i>. Moreover, compounds <b>3h</b>, <b>3j</b> and <b>7</b> showed favourable activity against vancomycin-resistant <i>E. faecium</i>. Compounds <b>9f</b> and <b>14f</b> showed broad-spectrum antifungal activity against drug-resistant <i>Candida</i> strains, while ester <b>8f</b> showed good activity against <i>Candida auris</i> which was greater than fluconazole. Collectively, these data demonstrate that <i>N</i>-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.
Item Description:10.3390/antibiotics12020220
2079-6382

Similar Items