10 resultados para PHARMACEUTICAL INTEREST
em Universidade do Minho
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Advances in Intelligent Systems and Computing, 353
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[Excerpt] Purine nucleobases are essential biomolecules in living organisms. Playing several key roles in the cell, they have been a significant inspiration for drug design.1 Benzimidazole nucleus is an important pharmacophore in the development of molecules with pharmaceutical or biological interest. Benzimidazoles have been reported to display significant pharmacological activities such as antiulcer, antifungal, antiparkinson, anticancer and antibiotic.2 Fused structures incorporating these two scaffolds might be important for medicinal chemistry and, to the best of our knowledge, there are no reports of these systems in the literature. In particular, benzo[4,5]imidazo[2,1]purines seem to be novel and must be important target molecules in the heterocyclic synthesis. (...)
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Purpose: Higher myopic refractive errors are associated with serious ocular complications that can put visual function at risk. There is respective interest in slowing and if possible stopping myopia progression before it reaches a level associated with increased risk of secondary pathology. The purpose of this report was to review our understanding of the rationale(s) and success of contact lenses (CLs) used to reduce myopia progression. Methods: A review commenced by searching the PubMed database. The inclusion criteria stipulated publications of clinical trials evaluating the efficacy of CLs in regulating myopia progression based on the primary endpoint of changes in axial length measurements and published in peerreviewed journals. Other publications from conference proceedings or patents were exceptionally considered when no peer-review articles were available. Results: The mechanisms that presently support myopia regulation with CLs are based on the change of relative peripheral defocus and changing the foveal image quality signal to potentially interfere with the accommodative system. Ten clinical trials addressing myopia regulation with CLs were reviewed, including corneal refractive therapy (orthokeratology), peripheral gradient lenses, and bifocal (dual-focus) and multifocal lenses. Conclusions: CLs were reported to be well accepted, consistent, and safe methods to address myopia regulation in children. Corneal refractive therapy (orthokeratology) is so far the method with the largest demonstrated efficacy in myopia regulation across different ethnic groups. However, factors such as patient convenience, the degree of initial myopia, and non-CL treatments may also be considered. The combination of different strategies (i.e., central defocus, peripheral defocus, spectral filters, pharmaceutical delivery, and active lens-borne illumination) in a single device will present further testable hypotheses exploring how different mechanisms can reinforce or compete with each other to improve or reduce myopia regulation with CLs.
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Dissertação de mestrado em Economia Industrial e da Empresa
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A therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems.
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Tese de Doutoramento em Biologia de Plantas
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The supercritical fluid technology has been target of many pharmaceuticals investigations in particles production for almost 35 years. This is due to the great advantages it offers over others technologies currently used for the same purpose. A brief history is presented, as well the classification of supercritical technology based on the role that the supercritical fluid (carbon dioxide) performs in the process.
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Dissertação de mestrado em Química Medicinal
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Dissertação de mestrado em Genética Molecular