title: Trioxaquines: hybrid molecules for the treatment of malaria.
abstract: Artemisinin, with its 1,2,4-trioxane as active motif, is now the first-line treatment for multidrug-resistant malaria. The endoperoxide ring is essential for the antimalarial activity of artemisinin. Based on its mechanism of action, new hybrid molecules named trioxaquines with a dual mode of action have been designed. Trioxaquines are made by the covalent attachment of a trioxane, having alkylating ability, to a quinoline, known to easily penetrate within infected erythrocytes. This review discusses the importance of various hybrid molecules of artemisinin and 4-aminoquinoline in the treatment of malaria and the evolution of a trioxaquine hybrid as a promising antimalarial drug candidate.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow, India.
authors.forename: Shikha S
authors.initials: SS
authors.lastname: Chauhan
authors.forename: Moni
authors.initials: M
authors.lastname: Sharma
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004351:Drug Resistance; D004912:Erythrocytes / Q000469:parasitology; D006801:Humans; D008288:Malaria / Q000188:drug therapy* / Q000635:transmission
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D037621:Artemisinins; C031327:artemisinin; C001920:4-aminoquinoline