Rethinking Triazoles as Antifungals: Synthesis and Evaluation of New Triazole Derivatives

• Autor(a) principal: Vieira, Andreia Sofia da Costa
• Data de Publicação: 2017
• Tipo de documento: Dissertação
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10362/81407
• topic: antifungal agents; azoles; pyrimidines; transition metals

"In the last decades, fungal infections have become a serious problem, mainly due to the excessive use of this reduced number of drugs, leading to an increase of acquired resistances1. Therefore, it is urgent to develop new and more effective antifungal medicines. The main objective of this master's thesis was the development of novel antifungal drugs, based on triazoles and pyrimidines, combining two groups with antifungal properties, known to be active in combinatorial therapies, in a single molecule. For the synthesis of these compounds, Huisgen's 1,3-dipolar cycloaddition methodologies, catalyzed by copper2 or ruthenium3 were employed. 1,4- and 1,5-triazoles derived from AZT (azidothymidine) were synthesized successfully as well as their methylated triazolium salts. Similarly, 1,4-triazoles derived from 5-fluorouracil were synthesized, as well as one methylated derivative. In general, the synthesis of the azidothymidine derivatives presented higher yields than those of 5-fluorouracil.(...)"