Although we have at our disposal relatively low-cost drugs that can be prescribed for the treatment of malaria, the prevalence of resistant strains of the causative parasite has required the...

Plasmodium species are responsible for a high incidence of cases and resistance, even with several approved drugs. Quinoline derivatives are recognized as a source of active compounds, where tafenoquine has been recently approved. Cases of resistance and the indiscriminate use of anti-malarials against COVID-19 have negatively contributed to eradicating this disease. In this context, modifications at 2- or 4-amino positions from the quinoline scaffold or even its metal complexes have shown promising advances in the field, especially against resistant strains, such as 3D7, W2, D10, Dd2, K1 , and FCR-3. In this chapter, we discussed all aspects involving such compounds, presenting their results based on SAR analysis and recent contributions/advances involving this classic scaffold arising from nature.