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Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
Martín-Escolano, Rubén; Moreno-Viguri, Elsa; Santivañez-Veliz, Mery; Martin-Montes, Alvaro; Medina-Carmona, Encarnación; Paucar, Rocío; Marín, Clotilde; Azqueta, Amaya; Cirauqui, Nuria; Pey, Angel L; Pérez-Silanes, Silvia; Sánchez-Moreno, Manuel.
Afiliación
  • Martín-Escolano R; Departament of Parasitology , Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios De Granada/University of Granada , Severo Ochoa s/n , E-18071 Granada , Spain.
  • Moreno-Viguri E; Universidad de Navarra , Department of Organic and Pharmaceutical Chemistry, Instituto de Salud Tropical , Pamplona 31008 , Spain.
  • Santivañez-Veliz M; Universidad de Navarra , Department of Organic and Pharmaceutical Chemistry, Instituto de Salud Tropical , Pamplona 31008 , Spain.
  • Martin-Montes A; Departament of Parasitology , Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios De Granada/University of Granada , Severo Ochoa s/n , E-18071 Granada , Spain.
  • Medina-Carmona E; Department of Physical Chemistry, Faculty of Sciences , University of Granada , Av. Fuentenueva s/n , 18071 Granada , Spain.
  • Paucar R; Universidad de Navarra , Department of Organic and Pharmaceutical Chemistry, Instituto de Salud Tropical , Pamplona 31008 , Spain.
  • Marín C; Departament of Parasitology , Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios De Granada/University of Granada , Severo Ochoa s/n , E-18071 Granada , Spain.
  • Azqueta A; Universidad de Navarra , Department of Pharmacology and Toxicology , Pamplona 31008 , Spain.
  • Cirauqui N; Department of Pharmaceutical Sciences , Federal University of Rio de Janeiro , Rio de Janeiro 21949-900 , Brazil.
  • Pey AL; Department of Physical Chemistry, Faculty of Sciences , University of Granada , Av. Fuentenueva s/n , 18071 Granada , Spain.
  • Pérez-Silanes S; Universidad de Navarra , Department of Organic and Pharmaceutical Chemistry, Instituto de Salud Tropical , Pamplona 31008 , Spain.
  • Sánchez-Moreno M; Departament of Parasitology , Instituto de Investigación Biosanitaria (ibs.Granada), Hospitales Universitarios De Granada/University of Granada , Severo Ochoa s/n , E-18071 Granada , Spain.
J Med Chem ; 61(13): 5643-5663, 2018 07 12.
Article en En | MEDLINE | ID: mdl-29883536
Chagas disease is a potentially life-threatening and neglected tropical disease caused by Trypanosoma cruzi. One of the most important challenges related to Chagas disease is the search for new, safe, effective, and affordable drugs since the current therapeutic arsenal is inadequate and insufficient. Here, we report a simple and cost-effective synthesis and the biological evaluation of the second generation of Mannich base-type derivatives. Compounds 7, 9, and 10 showed improved in vitro efficiency and lower toxicity than benznidazole, in addition to no genotoxicity; thus, they were applied in in vivo assays to assess their activity in both acute and chronic phases of the disease. Compound 10 presented a similar profile to benznidazole from the parasitological perspective but also yielded encouraging data, as no toxicity was observed. Moreover, compound 9 showed lower parasitaemia and higher curative rates than benznidazole, also with lower toxicity in both acute and chronic phases. Therefore, further studies should be considered to optimize compound 9 to promote its further preclinical evaluation.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tripanocidas / Trypanosoma cruzi / Bases de Mannich Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: España Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tripanocidas / Trypanosoma cruzi / Bases de Mannich Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: España Pais de publicación: Estados Unidos