Search results for "Anti-biofilm"
showing 10 items of 11 documents
IN VITRO ANTI-STAPHYLOCOCCAL BIOFILM ACTIVITY OF SOME NATURAL PYRROLOMYCINS AND SYNTHETIC DERIVATIVES
2008
Development of a new indole derivative dry powder for inhalation for the treatment of biofilm-associated lung infections
2022
The aim of this work was to produce an inhalable dry powder formulation of a new anti-biofilm compound (SC38). For this purpose, chitosan was used as a polymeric carrier and l-leucine as a dispersibility enhancer. SC38 was entrapped by spray-drying into previously optimized chitosan microparticles. The final formulation was fully characterized in vitro in terms of particle morphology, particle size and distribution, flowability, aerodynamic properties, anti-biofilm activity and effects on lung cell viability. The SC38-loaded chitosan microparticles exhibited favorable aerodynamic properties with emitted and respirable fractions higher than 80 % and 45 % respectively. The optimized formulati…
Synthetic small molecules as anti-biofilm agents in the struggle against antibiotic resistance
2018
Abstract Biofilm formation significantly contributes to microbial survival in hostile environments and it is currently considered a key virulence factor for pathogens responsible for serious chronic infections. In the last decade many efforts have been made to identify new agents able to modulate bacterial biofilm life cycle, and many compounds have shown interesting activities in inhibiting biofilm formation or in dispersing pre-formed biofilms. However, only a few of these compounds were tested using in vivo models for their clinical significance. Contrary to conventional antibiotics, most of the anti-biofilm compounds act as anti-virulence agents as they do not affect bacterial growth. I…
2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent staphylococcal biofilm inhibitors.
2019
Abstract A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis ATCC 12228, and the Gram-negative strains Pseudomonas aeruginosa ATCC 15442 and Escherichia coli ATCC 25922. Many of these new compounds, were able to inhibit biofilm formation of the tested staphylococcal strains showing BIC50 lower than 10 μg/ml. In particular, derivatives 9c and 9h showed remarkable anti-biofilm activity against S. aureus ATCC 25923 with BIC50 values of 0.5 and 0.8 μg/ml, r…
3,4,5,3’,5’-pentabromo-2-(2’-hydroxybenzoyl) pyrrole: a potential lead compound as anti Gram-positive and anti biofilm agent
2005
The activity against Gram-positive bacteria of 3,4,5,3 ,5 -pentabromo-2-(2 -hydroxybenzoyl)pyrrole I, a synthetic anti-bacterial compound related to pyrrolomycins, was tested in vitro using seven reference bacterial strains and Staphylococcus epidermidis and Staphylococcus aureus preformed biofilms. Compound I was active against all strains tested, with minimum inhibitory concentration (MIC) values ranging from 0.002 to 0.097 mg/l and minimum bactericidal concentrations (MBCs) from 0.37 to 12.5 mg/l. Compound I was also active at low concentrations against preformed S. epidermidis and S. aureus biofilms.
Development of natural and synthetic compounds as kinase inhibitors targeting cancer cells and cancer stem cells
2023
Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
2012
Abstract Several new 4-diazopyrazole derivatives 6a – g and 9a – c were obtained by the reaction of 1-(R-substituted-phenyl)-3-(1,3-dimethyl-1 H -pyrazol-5-yl)ureas 5a – g and N -(1,3-dimethyl-1 H -pyrazol-5-yl)-2-(R-substituted-phenyl)acetamides 8a – c respectively with a sevenfold excess of nitrous acid in acetic acid solution. The compounds were assayed for their activity against the Staphylococcus aureus reference strains ATCC 25923, ATCC 29213 and ATCC 6538, as well as six veterinary strains. The best anti-staphylococcal profile was showed by [(R-substituted-phenyl)acetyl](4-diazonio-1,3-dimethyl-1 H -pyrazol-5-yl)azanides 9a , c . Compound 9c was also able at 3.1 μg mL −1 to inhibit o…
Inhibitors of antibiotic resistance mechanisms: clinical applications and future perspectives
2020
Bacterial strains responsible for antibiotic resistant infections are increasing in an alarming way and the evolution of resistance mechanisms seems to be unstoppable. In the past decade, many efforts have been made in order to counteract this phenomenon but very few compounds have reached clinical trials. The development of new classes of antibiotics able to overcome the main bacterial drug resistance mechanisms is urgently required to counter the imminent danger of a postantibiotic era.
Pyrrolomycins as potential anti-staphylococcal biofilms agents
2010
With the goal of discovering new anti-infective agents active against microbial biofilms, this investigation focused on some natural pyrrolomycins, a family of halogenated pyrrole antibiotics. In this study the anti-staphylococcal biofilm activity of pyrrolomycins C, D, F1, F2a, F2b, F3 and of the synthesized related compounds I, II, III were investigated. The susceptibility of six staphylococcal biofilms was determined by methyltiazotetrazolium staining. Most of the compounds were active at concentrations of 1.5 microg ml(-1) with significant inhibition percentages. A few of the compounds were active at the lowest screening concentration of 0.045 microg ml(-1). The population log reduction…