title: 4-aminoquinoline analogues and its platinum (II) complexes as antimalarial agents.
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.
authors.affiliation: Departamento de Parasitologia, Microbiologia e Imunologia, ICB, Universidade Federal de Juiz de Fora, Campus Universitário, Rua José Lourenço Kelmer, 36036-900 Juiz de Fora, Minas Gerais, Brazil.
authors.forename: Nicolli Bellotti
authors.initials: NB
authors.lastname: de Souza
authors.forename: Arturene M L
authors.initials: AM
authors.lastname: Carmo
authors.forename: Davi C
authors.initials: DC
authors.lastname: Lagatta
authors.forename: Márcio José Martins
authors.initials: MJ
authors.lastname: Alves
authors.forename: Ana Paula Soares
authors.initials: AP
authors.lastname: Fontes
authors.forename: Elaine Soares
authors.initials: ES
authors.lastname: Coimbra
authors.forename: Adilson David
authors.initials: AD
authors.lastname: da Silva
authors.forename: Clarice
authors.initials: C
authors.lastname: Abramo
mesh_terms: D000634:Aminoquinolines / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D000962:Antimalarials / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D002470:Cell Survival / Q000187:drug effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D017737:Macrophages, Peritoneal / Q000187:drug effects; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D010962:Plasmodium berghei / Q000187:drug effects
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D009944:Organoplatinum Compounds; C001920:4-aminoquinoline