title: Novel compounds to combat trypanosomatid infections: a medicinal chemical perspective.
abstract: BACKGROUND
  The current therapeutic arsenal against the kinetoplastids Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp. is clearly inadequate and underscores the urgent need to develop new effective, safe and cost-effective drugs.
  
  
  METHODS
  Accordingly, this review of patented products and processes using anti-kinetoplastid agents provides insight into the identification of novel or more refined drugs. In this review, we describe products developed in recent years for the treatment of human African trypanosomiasis, American trypanosomiasis and leishmaniasis from a medicinal chemical perspective.
  
  
  CONCLUSIONS
  Applications so far have looked only superficially for candidate anti-trypanosomatid drugs and are deficient in the final stages of drug development studies, i.e., tolerance/safety, selectivity, drug-resistance, scaling-up, pharmacokinetic and pharmacodynamic assays. The ultimate goal for production of agents with anti-HAT activity has been the development of dicationic agents with parasite DNA-binding activity. Another goal for control of human African trypanosomiasis as well as for Chagas disease and leishmaniasis is the development of protease inhibitors. It should also be noted that several recent studies describing promising targets and compounds have not yet been patented. An effort should be made by foundations, international health organizations and pharmaceutical corporations to support analysis and development of promising new chemotherapeutic agents for controlling the trypanosomiasis and leishmaniasis.
authors.affiliation: Grupo de Química Medicinal, Laboratorio de Química Orgánica-Instituto de Química Biológica-Facultad de Ciencias, Universidad de la República/Iguá 4225, Montevideo 11400, Uruguay. megonzal@fq.edu.uy
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000627:therapeutic use*; D014355:Chagas Disease / Q000188:drug therapy*; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects; D007896:Leishmaniasis / Q000188:drug therapy*; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy*
chemical_list: D000981:Antiprotozoal Agents