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In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives

dc.contributor.authorMoreno-Viguri, Elsa
dc.contributor.authorJimenez-Montes, Carmen
dc.contributor.authorMartin-Escolano, Ruben
dc.contributor.authorSantivanez-Veliz, Mery
dc.contributor.authorMartin-Montes, Alvaro
dc.contributor.authorAzqueta, Amaya
dc.contributor.authorJimenez-Lopez, Marina
dc.contributor.authorZamora Ledesma, Salvador
dc.contributor.authorCirauqui, Nuria
dc.contributor.authorLopez de Cerain, Adela
dc.contributor.authorMarin, Clotilde
dc.contributor.authorSanchez-Moreno, Manuel
dc.contributor.authorPerez-Silanes, Silvia
dc.contributor.authoraffiliation[Moreno-Viguri, Elsa] Univ Navarra, Inst Trop Hlth, Dept Organ & Pharmaceut Chem, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Santivanez-Veliz, Mery] Univ Navarra, Inst Trop Hlth, Dept Organ & Pharmaceut Chem, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Perez-Silanes, Silvia] Univ Navarra, Inst Trop Hlth, Dept Organ & Pharmaceut Chem, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Azqueta, Amaya] Univ Navarra, Dept Pharmacol & Toxicol, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Lopez de Cerain, Adela] Univ Navarra, Dept Pharmacol & Toxicol, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Azqueta, Amaya] Recinto Complejo Hosp Navarra, Navarra Inst Hlth Res, IdiSNA, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Lopez de Cerain, Adela] Recinto Complejo Hosp Navarra, Navarra Inst Hlth Res, IdiSNA, Pamplona 31008, Spain
dc.contributor.authoraffiliation[Jimenez-Montes, Carmen] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Martin-Escolano, Ruben] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Martin-Montes, Alvaro] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Jimenez-Lopez, Marina] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Zamora Ledesma, Salvador] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Marin, Clotilde] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Sanchez-Moreno, Manuel] Univ Granada, Hosp Univ Granada, Inst Invest Biosanitaria Ibs GRANADA, Dept Parasitol, E-18014 Granada, Spain
dc.contributor.authoraffiliation[Cirauqui, Nuria] Univ Fed Rio de Janeiro, Dept Pharmaceut Sci, BR-21949900 Rio De Janeiro, Brazil
dc.contributor.funderUniversity of Navarra
dc.contributor.funderFPU from the Ministry of Education of Spain
dc.contributor.funderFundacion Caja Navarra
dc.contributor.funderInstitute of Tropical Health from the University of Navarra
dc.contributor.funderSpanish Ministry of Science and Innovation (MICINN)
dc.contributor.funderMinistry of Economy and Competitiveness (MINECO)
dc.date.accessioned2023-02-12T02:21:12Z
dc.date.available2023-02-12T02:21:12Z
dc.date.issued2016-12-22
dc.description.abstractChagas disease is a neglected tropical disease with 6-7 million people infected worldwide, and there is no effective treatment. Therefore, there is an urgent need to continue researching in order to discover novel therapeutic alternatives. We present a series of arylaminoketone derivatives as Means of identifying new drugs to treat Chagas disease in the acute phase with greater activity, less toxicity, and a larger spectrum of action than that corresponding to the reference drug benznidazole. Indexes of high selectivity found in vitro formed the basis for later in vivo assays in BALB/c mice. Murine model results show that compounds 3, 4, 7, and 10 induced a remarkable decrease in parasitemia levels in acute phase and the parasitemia reactivation following immunosuppression, and curative rates were higher than with benznidazole. These high antiparasitic activities encourage us to propose these compounds as promising molecules for developing an easy to synthesize anti-Chagas agent.
dc.identifier.doi10.1021/acs.jmedchem.6b00784
dc.identifier.essn1520-4804
dc.identifier.issn0022-2623
dc.identifier.unpaywallURLhttps://dadun.unav.edu/bitstream/10171/48346/3/3.pdf
dc.identifier.urihttp://hdl.handle.net/10668/18897
dc.identifier.wosID390735500007
dc.issue.number24
dc.journal.titleJournal of medicinal chemistry
dc.journal.titleabbreviationJ. med. chem.
dc.language.isoen
dc.organizationInstituto de Investigación Biosanitaria ibs. GRANADA
dc.page.number10929-10945
dc.publisherAmer chemical soc
dc.rights.accessRightsopen access
dc.subjectIron superoxide-dismutase
dc.subjectPolymerase-chain-reaction
dc.subjectChagas-disease
dc.subjectPotential antidepressants
dc.subjectSerotonin transporter
dc.subjectImidazole rings
dc.subjectMaesa-balansae
dc.subjectForce-field
dc.subjectInfection
dc.subjectBenznidazole
dc.titleIn Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives
dc.typeresearch article
dc.type.hasVersionSMUR
dc.volume.number59
dc.wostypeArticle
dspace.entity.typePublication

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