Synthesis of new marinoquinoline derivatives substituted in the pyrrolic portion with potential antimalarial activity

• Grant number: 23/07078-7
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: August 01, 2023
• End date: July 31, 2024
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Carlos Roque Duarte Correia
• Grantee: Lara Ferraz dos Santos Ferreira
• Host Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil

Abstract

A class of compounds called marinoquinolines (MQs) is being studied currently due to their great biological potential in the fight against malaria. Malaria is a disease caused by species of the parasite Plasmodium spp, which is transmitted to humans through the bite of the female mosquito Anopheles, when infected by the causative agent of the disease. The study of new drugs that fight the disease is important and has been gaining currently highlight due to the resistance that the parasites have gained against the different drugs already inserted in the actual market, making the treatment ineffective. In addition, the available vaccine (RTS,S/AS01), is not effective against all the species of the parasite. That said, the development of new drugs is essential, since the present scenario has a high case of deaths caused by the illness. In 2021 alone, malaria caused the death of 619,000 people, according to the World Health Organization (WHO). In this way, this project proposes to synthesize and characterize several QMs, which will be obtained from 8 to 9 reactional steps. These substances will be submitted to in vitro evaluation in front of P. falciparum, in collaboration with Prof. Dr. Rafael Victorio Carvalho Guido, from the Institute of Physics of São Carlos of the University of São Paulo, and with these results, a structure-activity relationship (SAR) study of this class of substances will be carried out, which will allow the identification of prototype substances for future evaluation of mechanism of action and other more advanced trials.