1. Repositório Aberto da Universidade do Porto
  2. I3S - Instituto de Investigação e Inovação em Saúde
  3. I3S - Artigo em Revista Científica Internacional
Please use this identifier to cite or link to this item: https://hdl.handle.net/10216/118203
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dc.creatorLoureiro, I-
dc.creatorThoo-Lin, P-
dc.creatorRamos, I-
dc.creatorRoura, M-
dc.creatorPruvost, A-
dc.creatorPemberton, I-
dc.creatorLoukil, H-
dc.creatorMacDougall, J-
dc.creatorTavares, J-
dc.creatorCordeiro-da-Silva, A-
dc.creatorGraça, NA-
dc.creatorGaspar, L-
dc.creatorCosta, DM-
dc.date.accessioned2019-01-08T10:00:15Z-
dc.date.available2019-01-08T10:00:15Z-
dc.date.issued2016-
dc.identifier.issn0066-4804-
dc.identifier.urihttps://repositorio-aberto.up.pt/handle/10216/118203-
dc.description.abstractCurrent 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.-
dc.description.sponsorshipFEDER PT2020 provided funding to Nuno A. G. Graça, Luis Gaspar, David M. Costa, Inês Loureiro, Joana Tavares, and Anabela Cordeiro-da-Silva under grant number Research Unit 4293. Seventh Framework Pro-gramme (FP7) provided funding to Luis Gaspar, David M. Costa, Inês Loureiro, Isbaal Ramos, Meritxell Roura, Alain Pruvost, Iain Pemberton, Hadjer Loukil, Jane MacDougall, and Anabela Cordeiro-da-Silva under grant number 602773- KINDReD. Seventh Framework Programme (FP7) provided funding to Nuno A. G. Graça and Anabela Cordeiro-da-Silva under grant number 300103- NMTrypI. Ministry of Education andScience | Fundação para a Ciência e Tecnologia (FCT) provided funding to Luis Gaspar under grant number SFRH/BD/81604/2011. Ministry of Education and Science | Fundação para a Ciência e Tecnologia (FCT) provided funding to Joana Tavares under grant number FCT Investigator.-
dc.language.isoeng-
dc.publisherAmerican Society for Microbiology-
dc.relationinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F81604%2F2011/PT-
dc.relation.ispartofAntimicrobial Agents and Chemotherapy, vol.60(4), p. 2532-2536-
dc.rightsopenAccess-
dc.rights.urihttps://creativecommons.org/licenses/by-nc-sa/3.0/-
dc.subject.meshNeurons/cytology-
dc.subject.meshNeurons/drug effects-
dc.subject.meshNeurons/metabolism-
dc.subject.meshParasite Load-
dc.subject.meshPentamidine/pharmacology-
dc.subject.meshPrimary Cell Culture-
dc.subject.meshStructure-Activity Relationship-
dc.subject.meshSurvival Analysis-
dc.subject.meshTrypanocidal Agents/chemical synthesis-
dc.subject.meshTrypanosoma brucei brucei/drug effects-
dc.subject.meshTrypanosoma brucei brucei/growth & development-
dc.subject.meshTrypanosoma brucei brucei/metabolism-
dc.subject.meshTrypanosomiasis, African/drug therapy-
dc.subject.meshTrypanosomiasis, African/mortality-
dc.subject.meshTrypanosomiasis, African/parasitology-
dc.subject.meshTrypanosomiasis, African/pathology-
dc.subject.meshTrypanocidal Agents/pharmacology-
dc.subject.meshAnimals-
dc.subject.meshCell Line-
dc.subject.meshDrug Stability-
dc.subject.meshFemale-
dc.subject.meshHepatocytes/cytology-
dc.subject.meshHepatocytes/drug effects-
dc.subject.meshHepatocytes/metabolism-
dc.subject.meshHumans-
dc.subject.meshInhibitory Concentration 50-
dc.subject.meshLiver/drug effects-
dc.subject.meshLiver/metabolism-
dc.subject.meshMacrophages/cytology-
dc.subject.meshMacrophages/drug effects-
dc.subject.meshMacrophages/metabolism-
dc.subject.meshMice-
dc.subject.meshMice, Inbred BALB C-
dc.subject.meshMicrosomes, Liver/drug effects-
dc.subject.meshMicrosomes, Liver/metabolism-
dc.subject.meshMitochondria, Liver/drug effects-
dc.subject.meshMitochondria, Liver/metabolism-
dc.subject.meshNaphthalimides/chemical synthesis-
dc.subject.meshNaphthalimides/pharmacology-
dc.titleActivity of bisnaphthalimidopropyl derivatives against trypanosoma brucei-
dc.typeArtigo em Revista Científica Internacional-
dc.contributor.uportoInstituto de Investigação e Inovação em Saúde-
dc.identifier.doi10.1128/AAC.02490-15-
dc.relation.publisherversionhttps://aac.asm.org/content/60/4/2532.long-
Appears in Collections:I3S - Artigo em Revista Científica Internacional

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