Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei
| العنوان: | Activity of bisnaphthalimidopropyl derivatives against trypanosoma brucei |
|---|---|
| المؤلفون: | Inês Loureiro, Jane MacDougall, Isbaal. Ramos, Paul Kong Thoo-Lin, Meritxell Roura, Anabela Cordeiro-da-Silva, Alain Pruvost, Joana Tavares, David Costa, Hadjer Loukil, Nuno A. G. Graça, Luís Gaspar, Ian K. Pemberton |
| المساهمون: | Instituto de Investigação e Inovação em Saúde |
| المصدر: | Repositório Científico de Acesso Aberto de Portugal Repositório Científico de Acesso Aberto de Portugal (RCAAP) instacron:RCAAP |
| بيانات النشر: | American Society for Microbiology, 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | 0301 basic medicine, Pentamidine/pharmacology, Naphthalimides/pharmacology, Neurons/metabolism, Mitochondria, Liver, Microsomes, Liver/metabolism, Pharmacology, Parasite load, Parasite Load, Neurons/cytology, Mice, 0302 clinical medicine, Macrophages/drug effects, Drug Stability, Trypanocidal Agents/chemical synthesis, Liver/drug effects, Trypanosoma brucei brucei/drug effects, Pharmacology (medical), African trypanosomiasis, Trypanosoma brucei brucei/metabolism, Hepatocytes/cytology, Neurons, Mice, Inbred BALB C, biology, Trypanosoma brucei brucei/growth & development, Trypanocidal Agents, 3. Good health, Naphthalimides, Infectious Diseases, Liver, Microsomes, Liver, Female, Trypanosomiasis, African/parasitology, Hepatocytes/drug effects, medicine.drug, Liver/metabolism, 030231 tropical medicine, Trypanosoma brucei brucei, Primary Cell Culture, Mitochondria, Liver/metabolism, Trypanosoma brucei, Cell Line, 03 medical and health sciences, Structure-Activity Relationship, Inhibitory Concentration 50, Macrophages/metabolism, medicine, Mitochondria, Liver/drug effects, Structure–activity relationship, Animals, Humans, Experimental Therapeutics, Pentamidine, Trypanocidal agent, Naphthalimides/chemical synthesis, Trypanosomiasis, African/mortality, business.industry, Macrophages, Hepatocytes/metabolism, Macrophages/cytology, medicine.disease, biology.organism_classification, Neurons/drug effects, Survival Analysis, 030104 developmental biology, Trypanosomiasis, African, Cell culture, Trypanosomiasis, African/pathology, Immunology, Hepatocytes, Trypanosomiasis, African/drug therapy, Microsomes, Liver/drug effects, business, Trypanosomiasis, Trypanocidal Agents/pharmacology |
| الوصف: | 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. FEDER 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. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5fa525ec4ee871c187c8e2ab92ea4a7 https://repositorio-aberto.up.pt/handle/10216/118203 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....f5fa525ec4ee871c187c8e2ab92ea4a7 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |