title: Biotransformation and biocatalysis: roles and applications in the discovery of antimalarials.
abstract: Several strategies to discover new antimalarials have been proposed to augment and complement the conventional drug-discovery paradigm. One approach, which has not yet been fully exploited, is the use of drug biotransformation to identify new active molecules. This concept rests on the use of the biotransformation of drugs to their pharmacologically active metabolites. This approach has been used successfully in human chemotherapy, with the discovery and development of several metabolite-based drugs. This review looks at the contribution that biotransformations can play in antimalarial drug discovery.
authors.affiliation: Department of Chemistry & Institute of Infectious Disease & Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Nyaradzo T L
authors.initials: NT
authors.lastname: Chigorimbo-Murefu
authors.forename: Mathew
authors.initials: M
authors.lastname: Njoroge
authors.forename: Alexis
authors.initials: A
authors.lastname: Nzila
authors.forename: Stefan
authors.initials: S
authors.lastname: Louw
authors.forename: Collen
authors.initials: C
authors.lastname: Masimirembwa
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D055162:Biocatalysis; D001711:Biotransformation; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D010961:Plasmodium / Q000187:drug effects*
chemical_list: D000962:Antimalarials