Chapter Six - Multicomponent reactions: A mighty journey partner for infectious tropical disease drug discovery

• Autores: Diego Muñoz-Torrero, Rodolfo Lavilla Grifols, Francisco Javier Pérez Areales, Ouldouz Ghashghaie
• Localización: Annual reports in medicinal chemistry, ISSN 0065-7743, Vol 53, 2019, págs. 181-217
• Idioma: inglés
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• Resumen

  • Infectious tropical diseases such as malaria, tuberculosis, and the so-called neglected tropical diseases are causing tremendous suffering to millions of people and huge impact on national economies, seriously worsening life conditions in the poorest parts of the world, where these diseases are endemic. Despite the existence of drugs for most of these diseases, they are far from adequate. Lack of efficacy, toxicity, and emergence of pathogen resistance are among the most important flaws of currently available drugs. Thus, apart from improving prevention and vector control measures, there is an urgent need for developing new efficacious, safe, and inexpensive drugs that desirably feature novel chemotypes. Multicomponent reactions (MCRs), where three or more reactants are combined in a one-pot reaction, constitute a very powerful tool for such endeavors, inasmuch as they enable a very rapid access to structurally diverse, usually complex scaffolds, shortening the synthesis of the novel drugs and, hence, lowering production costs, and affording original chemotypes. In this chapter, we provide an overview of the application of different types of MCRs to drug discovery against infectious tropical diseases, with particular emphasis on how structural complexity and molecular diversity can be readily introduced through their use.