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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

[en] AU(III), CU(II) AND BI(III) COMPLEXES OF FLUOROQUINOLONES: SYNTHESES, CHARACTERIZATION AND BIOLOGICAL ACTIVITY / [pt] COMPLEXOS DE AU(III), CU(II) E BI(III) DE FLUORQUINOLONAS: SÍNTESES, CARACTERIZAÇÃO FÍSICO-QUÍMICA E ATIVIDADE BIOLÓGICA

08 November 2021 (has links)
[pt] As fluorquinolonas constituem uma importante classe de agentes antimicrobianos sintéticos utilizados clinicamente por mais de 30 anos. Além da atividade antibacteriana, algumas fluorquinolonas, assim como seus complexos metálicos, mostraram ter atividade citotóxica, sendo, portanto, promissores como agentes antitumorais. Neste trabalho, obtivemos complexos de Au(III), Cu(II) e Bi(III) com as seguintes fluorquinolonas: norfloxacina, levofloxacina e esparfloxacina. Esses novos complexos foram caracterizados por diversas técnicas, tais como: análise elementar, condutimetria, espectroscopia na região do infravermelho, ressonância paramagnética eletrônica (RPE), ressonância magnética nuclear (RMN) de 1H e 13C, espectroscopia UV-Vis, fluorescência estacionária e resolvida no tempo. Atividades biológicas foram realizadas para todos os complexos. Usualmente, as fluorquinolonas coordenam-se aos íons metálicos de modo bidentado, através da carbonila do ácido carboxílico e da carbonila cetônica. Esta coordenação foi confirmada para os complexos de Cu(II), entretanto, para os complexos de Au(III) e Bi(III), os resultados de infravermelho e do RMN de 1H e 13C mostraram que a coordenação foi feita através dos nitrogênios do anel piperazina, uma coordenação não encontrada usualmente para as fluorquinolonas. Os complexos de Au(III) mostraram ser ativos frente às linhagens tumorais A20 (Linfoma murino), B16-F10 (Melanoma murino) e K562 (Leucemia mielóide humana). Os complexos de Cu(II) mostraram significativa atividade antiparasitária, enquanto os complexos de Bi(III), mostraram atividade antibacteriana. / [en] The fluoroquinolones are an important class of synthetic antimicrobial agents clinically used for over 30 years. In addition to antibacterial activity, some fluoroquinolones, as well as their metal complexes, presented cytotoxic activity and are therefore promising as antitumor agents. In order to obtain new complexes of Au (III) and other metal ions that have biological activity, this work had the objective to synthesize new complexes using ligands of the group of fluoroquinolones. These new complexes were characterized by various techniques such as elemental analysis, conductometry, infrared spectroscopy, electron paramagnetic resonance (EPR), nuclear magnetic resonance (NMR) of 1H and 13C NMR, UV-Vis, stead state and time-resolved fluorimetry studies. Biological activities were analized for all complexes. Usually, the fluoroquinolones coordinate to the metal ions as bidentate through the carbonyl and carboxylic acid ketonic carbonyl group. This was confirmed Cu(II) complex, however, for Au(III) and Bi (III) complexes, the results of IR and 1H and 13C NMR showed that the coordination was trough the nitrogen using the piperazine ring, a coordination not usually found for fluoroquinolones. The complexes of Au(III) shown to be active against the A20 tumor cell lines (murine lymphoma), B16-F10 (murine melanoma) and K562 (human myeloid leukemia). Complexes of Cu(II) showed significant antiparasitic activity, whereas complexes of Bi(III) have shown antibacterial activity.

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