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1.
J Med Chem ; 67(6): 4298-4321, 2024 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-38470824

RESUMO

The progressive increase in fungal infections and the decrease in the effectiveness of current therapy explain research on new drugs. The synthesis of compounds with proven antifungal activity, favorable physicochemical and pharmacokinetic properties affecting their pharmaceutical availability and bioavailability, and limiting or eliminating side effects has become the goal of many studies. The publication describes the directions of searching for new compounds with antifungal activity, focusing on conjugates. The described modifications include, among others, azoles or amphotericin B in combination with fatty acids, polysaccharides, proteins, and synthetic polymers. The benefits of these combinations in terms of activity, mechanism of action, and bioavailability were indicated. The possibilities of creating or using nanoparticles, "umbrella" conjugates, siderophores (iron-chelating compounds), and monoclonal antibodies were also presented. Taking into account the role of vaccinations in prevention, the scope of research related to developing a vaccine protecting against fungal infections was also indicated.


Assuntos
Antifúngicos , Micoses , Humanos , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Antifúngicos/química , Anfotericina B , Micoses/tratamento farmacológico , Azóis/uso terapêutico , Ácidos Graxos
2.
J Pharm Sci ; 111(9): 2471-2480, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35341720

RESUMO

Copper (II) histidinate injection solution, applied in Menkes disease treatment, is characterized by low stability due to sensitivity to oxidation. The aim of this article was to determine the critical points of the injection preparation procedure, taking into account selection of appropriate packaging, determining the solution pH or application of an excess of L-histidine. In order to assess the stability of the Cu(His)2 complex, the spectrophotometric method (VIS: 400-800 nm), and the colorimetric method using a reflectance colorimeter were applied. The color changes observed using the CIELAB color system made it possible to determine: the differences in the observed color (ΔΕ) and the color chroma (C*) and hue (h°). It was found that the following parameters: λmax and ΔE enable fast and objective assessment of copper (II) histidinate injection solution quality. The advantage of the colorimetric method is the non-invasiveness of the analysis which is performed through the packaging material (transparent vial). The developed methodology of preparing Cu(His)2 injections in hospitals or community pharmacies guarantees their stability for at least 6 months, provided that the solution is stored at lower temperatures (2-8°C or 4°C).


Assuntos
Cobre , Histidina , Cor , Colorimetria/métodos , Espectrofotometria
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