Last Updated: 07/07/2025
Discovery of 4-quinolinone derivatives as leading compound candidates for the development of new antimalarials
Objectives
*Original title in Portuguese: Descoberta de derivados 4-quinolinonas como candidatos a composto líder para o desenvolvimento de novos antimaláricos
The research project aims at the discovery and development of 4-quinolinone derivatives as candidates for a leading compound for the development of new antimalarial drugs.
Malaria, caused by protozoa of the genus Plasmodium, is one of the main public health problems in the world. The disease occurs in 91 countries, being endemic in tropical and subtropical regions of Africa, Southeast Asia and Latin America. Almost half of the world’s population (3 billion people) is exposed to malaria transmission in areas at risk. In 2015, 212 million cases and 429 thousand deaths were registered, most of them in Africa (WHO, 2016). The emergence of cases of resistance to available drugs makes it extremely important to develop new chemotherapeutic agents against the disease. For that, studies of cell biology and parasitology will be employed. The compounds will be evaluated in standardized biological tests against sensitive and resistant strains to the available drugs. In addition, cytotoxicity tests will be performed to determine the toxicological profile of the compounds. Preliminary results indicated that 4-quinolinone derivatives are promising inhibitors of Plasmodium falciparum in vitro. The work to be developed in this Scientific Initiation project will be of extreme value to the candidate’s scientific training with regard to the use of experimental methods for the discovery of new candidates for antimalarial drugs. The São Carlos Institute of Physics – USP has world-renowned experience in medicinal chemistry that was reinforced by the creation of the Research and Innovation Center on Biodiversity and Pharmaceuticals (CIBFar-CEPID), providing modern facilities for the discovery of new drug candidates. In addition, the group is part of the network of partner laboratories of the non-profit organization Medicine for Malaria Venture (MMV) as a Center for Screening and Evaluation of Candidates for Antimalarial Drugs. Therefore, the CIBFar-CEPID laboratories have complete infrastructure to carry out all the steps proposed in this research project.
Apr 2017 — Dec 2017
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