Please use this identifier to cite or link to this item:
https://hdl.handle.net/10216/118203| Author(s): | Loureiro, I Thoo-Lin, P Ramos, I Roura, M Pruvost, A Pemberton, I Loukil, H MacDougall, J Tavares, J Cordeiro-da-Silva, A Graça, NA Gaspar, L Costa, DM |
| Title: | Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei |
| Publisher: | American Society for Microbiology |
| Issue Date: | 2016 |
| Abstract: | Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives against Trypanosoma brucei. BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showed in vitro inhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration. |
| DOI: | 10.1128/AAC.02490-15 |
| URI: | https://repositorio-aberto.up.pt/handle/10216/118203 |
| Source: | Antimicrobial Agents and Chemotherapy, vol.60(4), p. 2532-2536 |
| Related Information: | info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F81604%2F2011/PT |
| Document Type: | Artigo em Revista Científica Internacional |
| Rights: | openAccess |
| License: | https://creativecommons.org/licenses/by-nc-sa/3.0/ |
| Appears in Collections: | I3S - Artigo em Revista Científica Internacional |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| Graça2016.pdf | 704.59 kB | Adobe PDF |  View/Open |
This item is licensed under a Creative Commons License
