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

6533b7d0fe1ef96bd125ba43

RESEARCH PRODUCT

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

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

subject

thiazole derivative Aquatic Organisms Staphylococcus aureus Indoles antibiotic resistance Settore BIO/05 - Zoologia Pharmaceutical Science Microbial Sensitivity Tests Bacterial growth Settore BIO/19 - Microbiologia Generale medicine.disease_cause 01 natural sciences Article nortopsentin Analytical Chemistry Microbiology lcsh:QD241-441 Inhibitory Concentration 50 chemistry.chemical_compound Alkaloids Antibiotic resistance lcsh:Organic chemistry Drug Discovery medicine Physical and Theoretical Chemistry Thiazole Strain (chemistry)010405 organic chemistry Pseudomonas aeruginosa marine alkaloids analogues Alkaloid Organic Chemistry Imidazoles Biofilm antibiofilm agents Settore CHIM/08 - Chimica Farmaceutica marine alkaloids analogue antibiofilm agent 0104 chemical sciences Thiazoles 010404 medicinal & biomolecular chemistry chemistry Chemistry (miscellaneous)Staphylococcus aureus Biofilms Pseudomonas aeruginosa thiazole derivatives Molecular Medicine

description

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 &micro

year	journal	country	edition	language
2020-12-27	Molecules

https://doi.org/10.3390/molecules26010081