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showing 10 items of 8346 documents
Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation
2020
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 a…
Synthesis and anticancer activity of new thiazole nortopsentin analogues
2015
Thiazolium salts as catalysts for etherification reaction
2014
MODIFICATION OF HYDROPHOBIC SURFACE WITH POLYASPARTAMIDE-BASED POLYCATIONS FOR BIOMEDICAL APPLICATION
2013
A convenient way for the achievement of polymer-based solid materials for specific biomedical applications is grafting the appropriate macromolecules onto the surfaces in order to confer them specific properties. To date many approaches have been used to covalently modify polymeric surfaces, and among them chemoselective coupling reactions, usually referred as “click” reactions, gained much attention thanks to simple procedure with high reaction rate under mild reaction conditions (at normal temperature and pressure) [1]. In particular, radical-initiated thiol-yne “photo-click” chemistry has been demonstrated as an effective way to functionalize efficiently surfaces. This method gives also …
Synthesis, antiproliferative activity, and in silico insights of new 3-benzoylamino-benzo[ b ]thiophene derivatives
2014
A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low micromolar range. The most active compounds were tested in cell cycle perturbation experiments. A rapid accumulation of cells in the G2/M phase, with a concomitant reduction of cells in both the S and G0/G1 phases, was observed, suggesting that cell exposure to selected derivatives produces mitotic failure. To rationalize the biological results, the 3-benzoylamino-benzo[b]thiophenes were analyzed thro…
A competitive reactivity study on the oxidative cyclization of thiosemicarbazones into 1,3,4-thiadiazoles
2022
Abstract In order to obtain useful insights on the mechanism of formation of 2(3H)-imino-1,3,4-thiadiazoles by oxidative cyclization of aldehyde thiosemicarbazones with Cu(II) or Fe(III) salts, a competitive reactivity study was performed on a suitable set of diversely substituted substrates, by means of HPLC techniques. This approach enabled to exploit Hammett’s equation without performing otherwise difficult-to-run kinetic experiments. The results presented herein support the hypothesis that the formation of the thiadiazole ring is induced by the attack of the oxidizing Lewis acid metal cation onto the imine-like nitrogen atom of the thiosemicarbazone substrate. Beyond mechanistic interpr…
Gas-liquid-solid operation of a Long Draft Tube Self-ingesting Reactor (LDTSR)
2008
Gas-liquid stirred vessels are widely employed to carry out chemical reactions involving a gas reagent and a liquid phase. The usual way for introducing the gas stream into the liquid phase is through suitable distributors placed below the impeller. An interesting alternative is that of using “self ingesting” vessels where the headspace gas phase is injected and dispersed into the vessel through suitable surface vortices. In this work the performance of a Long Draft Tube Self-ingesting Reactor dealing with gas-liquid-solid systems, is investigated. Preliminary experimental results on the effectiveness of this contactor for particle suspension and gas-liquid mass transfer performance in pres…
Mass transfer and hydrodynamic characteristics of a Long Draft Tube Self-ingesting Reactor (LDTSR) for gas-liquid-solid operations
2011
Gas-liquid stirred vessels are widely employed to carry out chemical reactions involving a gas reagent and a liquid phase. The usual way for introducing the gas stream into the liquid phase is through suitable distributors placed below the impeller. An interesting alternative is that of using “self ingesting” vessels where the headspace gas phase is injected and dispersed into the vessel through suitable surface vortices. In this work the performance of a Long Draft Tube Self-ingesting Reactor dealing with gas-liquid-solid systems, is investigated. Preliminary experimental results on the effectiveness of this contactor for particle suspension and gas-liquid mass transfer performance in pres…