| Autor: |
Wilson Cardona-G, Sara Maria Robledo, Laura Juliana Prieto, Andrés Felipe Yépes |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
Brazilian Journal of Pharmaceutical Sciences, Vol 58 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2175-9790 |
| DOI: |
10.1590/s2175-97902022e20822 |
| Popis: |
Abstract In order to overcome the challenges of discovering new antiprotozoal drugs, we synthesized a new class of hybrids based on S-allylCysteine Ester/Caffeic Acid Amide and evaluated four of them against Trypanosoma cruzi and Plasmodium falciparum. Hybrid 6 exhibited good activity on T. cruzi with an EC50 value of 5.45 µM, whereas hybrid 3 was active over P. falciparum with an EC50 of 18.08 µM. All hybrids displayed a good selectivity index on P. falciparum. Molecular docking computations indicated that several hybrids have good binding affinities towards the protozoa related enzymes (Cruzipain or Falcipain-2) when compared against current inhibitors. In silico studies showed that conjugates 1-3 and 6 fulfilled optimal ADME characteristics, suggesting them as safe alternatives for oral treatment of protozoal infections. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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