Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 M. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.

Anna Carbone, Stella Cascioferro, Barbara Parrino, Daniela Carbone, Camilla Pecoraro, Domenico Schillaci, et al. (2021). Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation. MOLECULES, 26(1), 1-16 [10.3390/molecules26010081].

Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

Anna Carbone;Stella Cascioferro;Barbara Parrino;Daniela Carbone;Camilla Pecoraro;Domenico Schillaci;Maria Grazia Cusimano;Girolamo Cirrincione;Patrizia Diana
2021

Abstract

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 M. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
Settore BIO/05 - Zoologia
Settore BIO/19 - Microbiologia Generale
Settore CHIM/08 - Chimica Farmaceutica
Anna Carbone, Stella Cascioferro, Barbara Parrino, Daniela Carbone, Camilla Pecoraro, Domenico Schillaci, et al. (2021). Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation. MOLECULES, 26(1), 1-16 [10.3390/molecules26010081].
File in questo prodotto:
File Dimensione Formato  
molecules-26-00081.pdf

accesso aperto

Descrizione: Articolo principale
Tipologia: Versione Editoriale
Dimensione 1.31 MB
Formato Adobe PDF
1.31 MB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10447/479917
Citazioni
  • ???jsp.display-item.citation.pmc??? 6
  • Scopus 18
  • ???jsp.display-item.citation.isi??? 18
social impact