title: Hits, leads and drugs against malaria through diversity-oriented synthesis.
abstract: Malaria is a devastating infectious disease and approximately half the world's population is at risk. Since vaccination is not yet available, small-molecule-based medicines are currently the best option for the treatment of patients suffering from malaria and combating the spread of infection. Development of resistance against existing drugs has created a need for new types of small molecules to be screened against Plasmodium falciparum, the etiological agent of malaria. The advent of diversity-oriented synthesis has enabled access to novel chemical structures. Evaluation of diversity-oriented synthesis compounds in phenotypic assays for growth inhibition of P. falciparum has resulted in novel hits, leads and even investigational drugs against malaria.
authors.affiliation: Chemical Biology Platform, Broad Institute, 7 Cambridge Center, Cambridge, MA 02142, USA.
authors.forename: Sivaraman
authors.initials: S
authors.lastname: Dandapani
authors.forename: Eamon
authors.initials: E
authors.lastname: Comer
authors.forename: Jeremy R
authors.initials: JR
authors.lastname: Duvall
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D010961:Plasmodium / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000962:Antimalarials