Last Updated: 30/07/2024
Synthesis of new marinoquinoline derivatives with potential antimalarial activity and determination of their molecular target
Objectives
This project proposes to synthesize and characterize several marinoquinolines (MQs), derived from the most powerful MQ ever discovered by Professor Correia’s group. Another objective of the project is to understand the mode of action of MQs, identifying the target of these compounds. With the target in hand, a molecular modeling study will be carried out to identify new potential structures, which will be synthesized and evaluated against P. falciparum.
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 with Plasmodium. According to the World Health Organization (WHO), in 2020 alone, malaria caused the death of 627,000 people. Currently, there are several drugs available on the market for the treatment of malaria, however, the parasites are gaining resistance to them, thus making the treatment ineffective. Furthermore, the only currently available vaccine (RTS,S/AS01) is not effective against all parasite species. Therefore, the development of new drugs capable of efficiently combating this disease is extremely urgent. In this context of drug discovery, a class of compounds called marinoquinolines (MQs) has been gaining prominence due to its inhibitory activities against Plasmodium. The proposed synthetic route involves 9 to 10 reaction steps, starting from pyrrole and 4-methoxy-2-nitroaniline. The new marinoquinolines will then be submitted to in vitro evaluation against P. falciparum.
Jul 2023 — Jun 2024
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