4-aminoquinoline analogues and its platinum (II) complexes as antimalarial agents

• Published in: Biomedicine & pharmacotherapy 2011-07, Vol.65 (4), p.313-316
• Main Authors: de Souza, Nicolli Bellotti, Carmo, Arturene M.L, Lagatta, Davi C, Alves, Márcio José Martins, Fontes, Ana Paula Soares, Coimbra, Elaine Soares, da Silva, Adilson David, Abramo, Clarice
• Format: Article
• Language: English
• Subjects: Aminoquinolines - adverse effects; Aminoquinolines - chemistry; Aminoquinolines - therapeutic use; Animals; Antimalarial activity; Antimalarials - adverse effects; Antimalarials - chemistry; Antimalarials - therapeutic use; Cell Survival - drug effects; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Design; Internal Medicine; Macrophages, Peritoneal - drug effects; Malaria - drug therapy; Malaria - parasitology; Medical Education; Mice; Molecular Structure; Organoplatinum Compounds - adverse effects; Organoplatinum Compounds - chemistry; Organoplatinum Compounds - therapeutic use; Plasmodium berghei; Plasmodium berghei - drug effects; Platinum (II) complexes; Quinoline
• ISSN: 0753-3322; 1950-6007
• DOI: 10.1016/j.biopha.2011.03.003

Abstract The high incidence of malaria and drug-resistant strains of Plasmodium have turned this disease into a problem of major health importance. One of the approaches used to control it is to search for new antimalarial agents, such as quinoline derivates. This class of compounds composes a broad group of antimalarial agents, which are largely employed, and inhibits the formation of β-haematin (malaria pigment), which is lethal to the parasite. More specifically, 4-aminoquinoline derivates represent potential sources of antimalarials, as the example of chloroquine, the most used antimalarial worldwide. In order to assess antimalarial activity, 12 4-aminoquinoline derived drugs were obtained and some of these derivatives were used to obtain platinum complexes platinum (II). These compounds were tested in vivo in a murine model and revealed remarkable inhibition of parasite multiplication values, whose majority ranged from 50 to 80%. In addition they were not cytotoxic. Thus, they may be object of further research for new antimalarial agents.