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Stability Characterization of Quinazoline Derivative BG1188 by Optical Methods

Militaru, Andra; Smarandache, Adriana; Mahamoud, Abdallah; Damian, Victor; Ganea, Paul; Alibert, Sandrine; Pages, Jean-Marie; Pascu, Mihail-Lucian


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    <subfield code="a">3-[2-(dimethylamino) ethyl]-6-nitroquinazolin-4(3H)-one, labeled BG1188, is a new synthesized compound, out of a series of quinazoline derivatives developed to fight the multidrug resistance of antibiotics acquired by bacteria. A characterization of the BG1188 powder was made using FTIR spectra in order to evidence the functional groups in the medicine's molecule. The ultraviolet-visible (UV-Vis) absorption spectra were used to study the stability of the BG1188 solutions in two solvents and at different temperatures. BG1188 concentration in ultrapure water was varied between 2x10(-3)M (stock solution) and 10(-6)M. The concentration recommended by higher activity on bacteria was 10(-3)M. For the same reason, this was the utilized concentration of BG1188 in dimethyl sulfoxide (DMSO). Time stability was characterized by comparing the time evolution of the UV-Vis absorption spectra of the BG1188 solutions in ultrapure deionized water or in DMSO. The spectra were recorded daily for about 4 months after the preparation for the BG1188 solutions in ultrapure water. Generally, samples are stable within the experimental errors at concentrations higher than 10(-5)M, but the stability time interval may vary from 119 days at 10(-4)M to 34 days at 10-5M. Time evolution of the absorption spectra at 10-3M in ultrapure water shows reproducibility within the measuring errors (+/- 1.045%) for time intervals up to 1032 hours (more than 40 days) after preparation. On the other hand, BG1188 solutions in DMSO may be considered unstable because the absorption spectra modify in terms of peak shapes and intensities, indicating that the samples exhibit modifications immediately after preparation. Regardless the solvent used, some aggregation phenomena took place and wire-like aggregates were observed in all the solutions with the naked eye. These aggregates were analyzed, tentatively, using optical microscopy and FTIR.</subfield>
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