Synthesis and antiprotozoal activity of furanchalcone-quinoline, furanchalcone-chromone and furanchalcone-imidazole hybrids

Joint Event on 3^rd World Chemistry Conference & World Congress on Biotherapeutics and Bioanalytical Techniques

September 11-12, 2017 Dallas, USA

Elisa Garcia, Juan C Coa, Miguel Carda, Ivan D Velez, Sara M Robledo and Wilson I Cardona

University of Antioquia, Colombia
Jaume I University, Spain

Posters & Accepted Abstracts: Chem Sci J

Abstract :

Statement of the Problem: Neglected tropical diseases (NTD) include, among others, Chagas���¢�������� disease (American trypanosomiasis) caused by parasitic protozoan Trypanosoma cruzi and leishmaniasis caused by Leishmania species. These diseases affect more than 10 million people worldwide. Current chemotherapies for those diseases are based on old drugs, such as pentavalent antimonials (Meglumine antimoniate and Sodium stibogluconate) to treat cutaneous leishmaniasis and nitroaromatic compounds (Benznidazole and Nifurtimox) for treatment of Chagas disease. Unfortunately, all these drugs are not very effective in the chronic phase and have toxicity, side effects and parasite resistance. Strategies for the discovery and development of new drugs are necessaries for the use in the treatment of parasitic diseases. In recent years, a promising strategy has emerged based on hybrid molecules which bear in their structures two distinct pharmacophores. This type of molecules could improve the bioavailability and absorption and could enhance the antiprotozoal activity due a synergic mechanism. In this work, we are going to show the synthesis and biological activities (cytotoxicity, leishmanicidal and trypanocidal) of several furanchalcone-quinoline, furanchalcone-chromone and furanchalcone-imidazole hybrids. The final compounds showed yields between 16-46% for furanchalcone-quinoline hybrids, 7-33% for furanchalcone-chromone and 39-98% for furanchalconeimidazole. The synthetized compounds were evaluated against intracellular amastigotes of L. panamensis, and intracellular amastigotes of Trypanosoma cruzi. Cytotoxicity was evaluated against human U-937 macrophages. Briefly, although these compounds showed high toxicity for mammalian U-937 cells, most of the compounds were very active against T. cruzi and L. panamensis. Four compounds showed a high activity against L. panamensis and five compounds exhibited high activity against T. cruzi, all of them with effective concentration 50 (EC50) less than 10 �������¼M. Furanchalcone-imidazole hybrids were the most active of all compounds, showing that the imidazole salt moiety is important for their biological actions.

Biography :

Elisa García has received her Undergraduate degree in Chemistry from the University of Antioquia. Currently, she is doing a Master's degree in Chemical Sciences at the same University. During her studies, she had the opportunity of being involved in diverse research fields such as Electrochemistry, Natural Products, Synthesis, and Organic Chemistry. Now, her research focuses on the synthesis of hybrid molecules as a potential Trypanosoma cruzi and Leishmania agents.
Email:eli.goc5@gmail.com