Time Stability Studies of Quinazoline Derivative Designed to Fight Drug Resistance Acquired by Bacteria
About: This article is published in Letters in Drug Design & Discovery.The article was published on 2011-01-31. It has received 8 citations till now.
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TL;DR: In this article, two quinazoline derivatives, labelled BG1189 and BG1190, were proposed as EPIs, and the pharmacodynamic and pharmacokinetic profile of these quinnazolines were investigated in silico approach.
Abstract: Multidrug resistance of bacteria is a worrying concern in the therapeutic field and an alternative method to combat it is designing new efflux pump inhibitors (EPIs). This article presents a molecular study of two quinazoline derivatives, labelled BG1189 and BG1190, proposed as EPIs. In silico approach investigates the pharmacodynamic and pharmacokinetic profile of BG1189 and BG1190 quinazolines. Molecular docking and predicted ADMET features suggest that BG1189 and BG1190 may represent attractive candidates as antimicrobial drugs. UV-Vis absorption spectroscopy was employed to study the time stability of quinazoline solutions in water or in dimethyl sulfoxide (DMSO), in constant environmental conditions, and to determine the influence of usual storage temperature, normal room lighting and laser radiation (photostability) on samples stability. The effects of irradiation on BG1189 and BG1190 molecules were also assessed through Fourier-transform infrared (FTIR) spectroscopy. FTIR spectra showed that laser radiation breaks some chemical bonds affecting the substituents and the quinazoline radical of the compounds.
16 citations
TL;DR: The wetting behaviour of CPZ, PZ and PMZ solutions, irradiated for time intervals between 1 and 240 min, on the surfaces of the three textures is reported in order to draw a conclusion about their wettability as a function of time.
9 citations
Cites background or methods from "Time Stability Studies of Quinazoli..."
...The corresponding error was calculated for the first characteristic peak of CPZ at 254 nm, according to (Militaru et al., 2011)....
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...characteristic peak of CPZ at 254 nm, according to (Militaru et al., 2011)....
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TL;DR: Chlorpromazine solutions irradiated for 15 min and 30’min have the best antimicrobial and antibiofilm activity against Staphylococcus aureus ATCC 6538, methicillin susceptible StaphYLococcusAureus, Methicillin resistant StAPHylococus aUREus, Enterococcus faecium 17-VAR, Enteritis faecalis 2921, and Bacillus subtilis 6633.
8 citations
TL;DR: The evolution of different antimicrobial drugs in terrestrial, microgravity and hypergravity conditions is presented within this review, in connection with their implementation during human space exploration as mentioned in this paper, in which schemes and procedures to find reliable ways of fighting multiple drug resistance acquired by microorganisms are provided.
Abstract: The evolution of different antimicrobial drugs in terrestrial, microgravity and hypergravity conditions is presented within this review, in connection with their implementation during human space exploration. Drug stability is of utmost importance for applications in outer space. Instabilities may be radiation-induced or micro-/hypergravity produced. The antimicrobial agents used in space may have diminished effects not only due to the microgravity-induced weakened immune response of astronauts, but also due to the gravity and radiation-altered pathogens. In this context, the paper provides schemes and procedures to find reliable ways of fighting multiple drug resistance acquired by microorganisms. It shows that the role of multipurpose medicines modified at the molecular scale by optical methods in long-term space missions should be considered in more detail. Solutions to maintain drug stability, even in extreme environmental conditions, are also discussed, such as those that would be encountered during long-duration space exploratory missions. While the microgravity conditions may not be avoided in space, the suggested approaches deal with the radiation-induced modifications in humans, bacteria and medicines onboard, which may be fought by novel pharmaceutical formulation strategies along with radioprotective packaging and storage.
5 citations
TL;DR: In this article, the rapid molecular changes induced by laser radiation on two novel hydantoin derivatives (SZ-2 and SZ-7) have been investigated, and the effect of exposure to laser radiation was highlighted by laser induced fluorescence.
3 citations
References
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TL;DR: Data suggest that polymyxin-resistant or PDR P. pneumoniae clinical isolates are currently relatively rare and the fears for the dawn of a post-antibiotic era appear to be justified, at least for these three Gram-negative bacteria.
376 citations
TL;DR: Recent data underscore that the impact of multidrug resistance on the outcome of nosocomial infection might differ depending on the study population, type of infection,type of pathogen and appropriateness of therapy, and hence, that any conclusion drawn prior to accurate accounting for imbalanced confounders is premature and potentially false.
Abstract: Purpose of reviewThe review examines potential confounders hampering measurement of the impact of multidrug resistance in nosocomial infections. Methodological techniques dealing with the problem of confounding are discussed and current findings in how multidrug resistance affects outcome in patient
102 citations