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.
Keywords: Drug discovery, Plasmodium spp, Quinoline-based, SAR analysis.
