This submission belongs to the session b. Bioorganic, Medicinal and Natural Products of the event The 16th International Electronic Conference on Synthetic Organic Chemistry
Published date
30 Oct, 2012
Citation
Lourdes Santana, Eugenio Uriarte, Fernanda Pérez-Cruz, Claudio Olea-Azar, Michel Lapier, Juan Diego Maya, Roberto Figueroa Guíñez, Maria João Matos, Saleta VazquezRodriguez, Coumarin-chalcone Derivatives as Potential Antitrypanosomal and Antioxidant Compounds, in Proceedings of The 16th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2012, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-16-01037
Share
Email
Facebook
Twitter
LinkedIn
Coumarin-chalcone Derivatives as Potential Antitrypanosomal and Antioxidant Compounds
Saleta VazquezRodriguez 1
Maria João Matos 1
Roberto Figueroa Guíñez 2
Juan Diego Maya 3
Michel Lapier 2
Claudio Olea-Azar 2
Fernanda Pérez-Cruz 2
Eugenio Uriarte 1
Lourdes Santana 1
1. Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782, Santiago de Compostela, Spain
2. Departamento de Química Inorgánica y Analítica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago, Chile
3. Departamento de Farmacología Molecular y Clínica, Facultad de Medicina, Universidad de Chile, Santiago, Chile
Abstract
Trypanosoma cruzi, the causative agent of Chagas\' disease, which is widely disseminated in Central and South America, represents an endemic neglected disease located in this geographic region. Therefore, there is an urgent need for the discovery of new, more effective, and safer drugs for human use. Natural products have played a major role in the chemotherapy of parasitic diseases. Based on the observed biological activities of two kind of natural compunds, coumarins and chalcones, we have synthesized coumarin-chalcone hybrids with the aim of evaluating their activity against Trypanosoma cruzi, and their antioxidant properties. All derivates have shown moderate trypanocidal activity in the epimastigote stage (clone Dm28c) being compound 3 the one with the highest activity. These preliminary findings encourage us to future structural optimization of this compound. In spite of the moderate trypanocidal activity of coumarin-chalcone hybrids, they have been proved to be very good antioxidants. Based on these results, we can conclude that compounds 3 and 4 are potential candidates for in vitro studies of their antioxidant activity.
Keywords
Coumarin
Chalcone
Antitrypanosomal
Antioxidant
Reactive Oxygen Species (ROS).
Synthesis of Novel Amino/Nitro Substituted 3-Arylcoumarins as Antibacterial Agents
A Facile Synthesis of -N-Ribosyl-Asparagine and -N-Ribosyl-Glutamine Building Blocks