Novel [1,3,4]Thiadiazole[3,2- a ]pyrimidin-5-ones as Promising Biofilm Dispersal Agents against Relevant Gram-Positive and Gram-Negative Pathogens

Biofilm-associated infections pose significant challenges in healthcare settings due to their resistance to conventional antimicrobial therapies. In the last decade, the marine environment has been a precious source of bioactive molecules, including numerous derivatives with antibiofilm activity. In...

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Bibliographic Details
Published in:Marine drugs 2024-03, Vol.22 (3), p.133
Main Authors: Carbone, Daniela, Pecoraro, Camilla, Scianò, Fabio, Catania, Valentina, Schillaci, Domenico, Manachini, Barbara, Cascioferro, Stella, Diana, Patrizia, Parrino, Barbara
Format: Article
Language:English
Subjects:
anti-biofilm agents
Antibiotics
Antiinfectives and antibacterials
Biocompatibility
Biofilms
Biological Assay
Candida albicans
Cells
Composition
Control
dispersal activity
Dispersion
Dosage and administration
Drug resistance in microorganisms
E coli
Fungi
Galleria mellonella
Hybridization
Hybridization, Genetic
Identification and classification
Marine environment
Microbial mats
Microbiological strains
Microorganisms
nortopsentin analogs
Pandemics
Pathogens
Permeability
Prevention
Staphylococcus infections
Thiadiazoles
thiadiazopyrimidinone derivatives
Toxicity
Virulence
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Summary:Biofilm-associated infections pose significant challenges in healthcare settings due to their resistance to conventional antimicrobial therapies. In the last decade, the marine environment has been a precious source of bioactive molecules, including numerous derivatives with antibiofilm activity. In this study, we reported the synthesis and the biological evaluation of a new series of twenty-two thiadiazopyrimidinone derivatives obtained by using a hybridization approach combining relevant chemical features of two important classes of marine compounds: nortopsentin analogues and Essramycin derivatives. The synthesized compounds were in vitro tested for their ability to inhibit biofilm formation and to disrupt mature biofilm in various bacterial strains. Among the tested compounds, derivative exhibited remarkable dispersal activity against preformed biofilms of relevant Gram-positive and Gram-negative pathogens, as well as towards the fungus , showing BIC values ranging from 17 to 40 µg/mL. Furthermore, compound was in vivo assayed for its toxicity and the anti-infective effect in a model. The results revealed a promising combination of anti-infective properties and a favorable toxicity profile for the treatment of severe chronic biofilm-mediated infections.
ISSN:1660-3397
1660-3397
DOI:10.3390/md22030133