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DESIGN AND SYNTHESIS OF NEW STEROID DERIVATIVES WITH ANTIMALARIAL POTENTIAL

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Resumo:Malaria is a life-threatening disease being accountable for over half a million fatalities every year, being control and elimination hindered by the capacity of Plasmodium falciparum to develop antimalarial drug resistance. The efficacy of artemisinin-based combination therapies (ACT) contributed to a decrease in malaria mortality, nevertheless, resistance is a reality. Being ACT efficacy threatened, efforts to identify the molecular basis of multidrug resistance and discover new compound classes, ideally with novel mechanisms of action, are desperatly needed. Natural compounds, such as steroids, have emerged as attractive scaffolds for drug discovery due to their diverse biological activities. Supplementing previous findings from our group on the antimalarial properties of steroidal derivatives, the primary goals of this thesis were to design and synthesize new steroid-based compounds and to fully characterize their chemical structures.A total of ten steroid derivatives that included diferrent substituents at rings A, B, and D were synthesized in order to further explore the potential of this scaffold as a platform for the design of novel antimalarial drugs. Although biological evaluation of these compounds could not be carried out within the timeframe of this thesis, such assays are planned for the near future. Altogether, this work contributes to a new panel of steroidal derivatives to the pipeline of potential antimalarial agents and offers a starting point for subsequent biological screening and structure-activity relationship studies.
Autores principais:Ribeiro, Carina Calixto
Assunto:Malaria Plasmodium falciparum Drug resistance Synthetic steroids Drug Discovery Malária Plasmodium falciparum Resistência a fármacos Esteroides sintéticos Descoberta de fármacos
Ano:2025
País:Portugal
Tipo de documento:dissertação de mestrado
Tipo de acesso:acesso embargado
Instituição associada:Universidade de Coimbra
Idioma:inglês
Origem:Estudo Geral - Universidade de Coimbra

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