Publication: In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives
dc.contributor.author | Moreno-Viguri, Elsa | |
dc.contributor.author | Jimenez-Montes, Carmen | |
dc.contributor.author | Martin-Escolano, Ruben | |
dc.contributor.author | Santivanez-Veliz, Mery | |
dc.contributor.author | Martin-Montes, Alvaro | |
dc.contributor.author | Azqueta, Amaya | |
dc.contributor.author | Jimenez-Lopez, Marina | |
dc.contributor.author | Zamora Ledesma, Salvador | |
dc.contributor.author | Cirauqui, Nuria | |
dc.contributor.author | Lopez de Cerain, Adela | |
dc.contributor.author | Marin, Clotilde | |
dc.contributor.author | Sanchez-Moreno, Manuel | |
dc.contributor.author | Perez-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.funder | University of Navarra | |
dc.contributor.funder | FPU from the Ministry of Education of Spain | |
dc.contributor.funder | Fundacion Caja Navarra | |
dc.contributor.funder | Institute of Tropical Health from the University of Navarra | |
dc.contributor.funder | Spanish Ministry of Science and Innovation (MICINN) | |
dc.contributor.funder | Ministry of Economy and Competitiveness (MINECO) | |
dc.date.accessioned | 2023-02-12T02:21:12Z | |
dc.date.available | 2023-02-12T02:21:12Z | |
dc.date.issued | 2016-12-22 | |
dc.description.abstract | Chagas 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.doi | 10.1021/acs.jmedchem.6b00784 | |
dc.identifier.essn | 1520-4804 | |
dc.identifier.issn | 0022-2623 | |
dc.identifier.unpaywallURL | https://dadun.unav.edu/bitstream/10171/48346/3/3.pdf | |
dc.identifier.uri | http://hdl.handle.net/10668/18897 | |
dc.identifier.wosID | 390735500007 | |
dc.issue.number | 24 | |
dc.journal.title | Journal of medicinal chemistry | |
dc.journal.titleabbreviation | J. med. chem. | |
dc.language.iso | en | |
dc.organization | Instituto de Investigación Biosanitaria ibs. GRANADA | |
dc.page.number | 10929-10945 | |
dc.publisher | Amer chemical soc | |
dc.rights.accessRights | open access | |
dc.subject | Iron superoxide-dismutase | |
dc.subject | Polymerase-chain-reaction | |
dc.subject | Chagas-disease | |
dc.subject | Potential antidepressants | |
dc.subject | Serotonin transporter | |
dc.subject | Imidazole rings | |
dc.subject | Maesa-balansae | |
dc.subject | Force-field | |
dc.subject | Infection | |
dc.subject | Benznidazole | |
dc.title | In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives | |
dc.type | research article | |
dc.type.hasVersion | SMUR | |
dc.volume.number | 59 | |
dc.wostype | Article | |
dspace.entity.type | Publication |