Last Updated: 30/07/2024
Synthesis of new marinoquinoline derivatives substituted in the pyrrolic moiety with potential antimalarial activity
Objectives
In this proposal a study of the structure-activity relationship (REA) of marinoquinoline derivatives substituted in the pyrrolic moiety will be carried out, which will allow identifying prototype substances for future mechanism of action evaluations and other more advanced assays.
A class of compounds called marinoquinolines (MQs) is currently being studied due to their great biological potential in combating malaria. Malaria is a disease caused by species of the parasite Plasmodium spp, which is transmitted to humans through the bite of the female Anopheles mosquito, when infected by the agent that causes the disease. The study of new medicines that combat the disease is extremely important and is currently gaining prominence due to the resistance that the parasites have gained against the different drugs already on the current market, making the treatment ineffective. Furthermore, the currently available vaccine (RTS,S/AS01) is not effective against all species of the parasite. That said, the development of new medicines is essential, given that the current scenario has a high number of deaths caused by the disease; In 2021 alone, malaria caused the deaths of 619,000 people, according to the World Health Organization (WHO). Therefore, this project proposes to synthesize and characterize several MQs, which will be obtained from 8 to 9 reaction steps. These substances will be subjected to in vitro evaluation against P. falciparum, in collaboration with Prof. Dr. Rafael Victorio Carvalho Guido, from the São Carlos Institute of Physics at the University of São Paulo.
Aug 2023 — Jul 2024
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