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New multicomponent reactions to design active compounds against trypanosomiasis

Date:
July 12, 2016
Source:
Universidad de Barcelona
Summary:
Multicomponent reactions are protocols that ease the chemical synthesis of new compounds, and are particularly important to gain molecules with biological activity as therapeutic agents against several pathogens. New scientific work on multicomponent reactions to find new active compounds against parasites causing trypanosomiasis has now been published by researchers.
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FULL STORY

Multicomponent reactions are protocols that ease the chemical synthesis of new compounds, and are particularly important to gain molecules with biological activity as therapeutic agents against several pathogens. The journal Angewandte Chemie International Edition has published new scientific work on multicomponent reactions to find new active compounds against parasites causing trypanosomiasis.

The new research project is led by Professor Rodolfo Lavilla, from the Department of Pharmacology, Toxicology and Therapeutic Chemistry of the Faculty of Pharmacy and Food Sciences of the University of Barcelona, and member of the group ChemBioLab (UB) with headquarters in the Barcelona Science Park (PCB)

Human African Trypanosomiasis -- also known as sleeping sickness -- is a parasitic disease transmitted by the tsetse fly and provoked by Trypanosoma protozoans. It exists in around 40 countries of the sub-Saharan Africa and in more than 98% of the cases the parasite causing the disease is the Trypanosoma brucei gambiense. Regarding the American trypanosomiasis or Chagas disease, transmitted by bedbugs, between 6 and 7 million people are infected by the pathogen (Trypanosoma cruzi), most of them are in Latin America.

A more direct and efficient synthesis methodology

Multicomponent reactions are very direct and simple. The new processes developed by the research team are based on classic heterocyclic chemistry, and in ideal conditions, they allow reaching the complete synthesis in just one stage. They are versatile, and allow obtaining a wide collection of products and selecting the compound with better biological and physicochemical characteristics as a drug.

The new preclinical study shows the in vitro performance of the new compounds against the Trypanosoma brucei and T. Cruzi parasites. According to Rodolfo Lavilla, "one of the new factors of the new reactivity is that, apart from allowing an efficient synthesis, it represents a new way of activation of compounds that are essential in multicomponent reactions, the isonitrils."

According to the authors of the study, in future researches it will be necessary to know about the action mechanism of the new products -highly selective and with low cell toxicity on in vitro tests- and broaden preclinical studies with laboratory animal models.

In the new interdisciplinary work of the journal Angewandte Chemie International Edition, with the collaboration of the Department of Nutrition, Food Science and Gastronomy of the University of Barcelona (computational chemistry); Rocío Gámez-Montaño, from the University of Guanajato in Mexico (synthesis and mechanism model); John M. Kelly from the London School of Hygiene and Tropical Medicine of the United Kingdom (biological studies on anti-parasite activity), and Diego Muñoz-Torrero from the Department of Pharmacology, Therapeutics and Toxicology of the UAB, in the field of chemic compound pharmacy.


Story Source:

Materials provided by Universidad de Barcelona. Note: Content may be edited for style and length.


Journal Reference:

  1. Kranti G. Kishore, Ouldouz Ghashghaei, Carolina Estarellas, M. Mar Mestre, Cristina Monturiol, Nicola Kielland, John M. Kelly, Amanda Fortes Francisco, Shiromani Jayawardhana, Diego Muñoz-Torrero, Belén Pérez, F. Javier Luque, Rocío Gámez-Montaño, Rodolfo Lavilla. Insertion of Isocyanides into N−Si Bonds: Multicomponent Reactions with Azines Leading to Potent Antiparasitic Compounds. Angewandte Chemie, 2016; DOI: 10.1002/ange.201604109

Cite This Page:

Universidad de Barcelona. "New multicomponent reactions to design active compounds against trypanosomiasis." ScienceDaily. ScienceDaily, 12 July 2016. <www.sciencedaily.com/releases/2016/07/160712093924.htm>.
Universidad de Barcelona. (2016, July 12). New multicomponent reactions to design active compounds against trypanosomiasis. ScienceDaily. Retrieved May 8, 2017 from www.sciencedaily.com/releases/2016/07/160712093924.htm
Universidad de Barcelona. "New multicomponent reactions to design active compounds against trypanosomiasis." ScienceDaily. www.sciencedaily.com/releases/2016/07/160712093924.htm (accessed May 8, 2017).