Alkaloids and Other Nitrogen-Containing Derivatives

Design of Antimalarial Compounds on Quinoline Scaffold: From Plant to Drug

Author(s): Paulo F. S. Santos-Júnior, Igor J. S. Nascimento, Geraldo J. S. Neto, Rafael J. M. Omena, Thiago M. Aquino, João X. Araújo-Júnior, Mario R. Meneghetti and Edeildo F. Silva-Júnior * .

Pp: 189-237 (49)

DOI: 10.2174/9789815123678123030010

* (Excluding Mailing and Handling)


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.

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