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dc.creatorGualdesi, María Soledad-
dc.creatorOrtiz, Cristina Susana-
dc.creatorRaviolo, Mónica Ana-
dc.date2019-02-04T17:34:29Z-
dc.date2019-02-04T17:34:29Z-
dc.date2016-01-
dc.date2019-02-04T13:02:48Z-
dc.date.accessioned2019-04-29T15:46:30Z-
dc.date.available2019-04-29T15:46:30Z-
dc.date.issued2016-01-
dc.identifierGualdesi, María Soledad; Ortiz, Cristina Susana; Raviolo, Mónica Ana; Synthesis and pharmaceutical properties of N-acyloxymethyl prodrugs of Allop with potential anti-trypanosomal activity; Taylor ; Drug Development and Industrial Pharmacy; 42; 4; 1-2016; 602-610-
dc.identifier0363-9045-
dc.identifierhttp://hdl.handle.net/11336/69296-
dc.identifierCONICET Digital-
dc.identifierCONICET-
dc.identifier.urihttp://rodna.bn.gov.ar:8080/jspui/handle/bnmm/301664-
dc.descriptionWe report herein the synthesis, and the physicochemical and pharmacokinetic properties of N-acyloxymethyl prodrugs of allopurinol (Allop) (2a-f). Allop is a compound with activity against Trypanosoma cruzi, a causative agent of Chagas disease. Its pathology leads to a huge number of infections and deaths per year, because in addition to many sufferers only having limited access to health services only an inefficient chemotherapy is available. Relevant pharmaceutical properties (pKa, stability, solubility, lipophilicity, in vitro permeability, binding protein, xanthine oxidase binding) were also determined. The results obtained showed that derivatives behave as prodrugs of Allop, since they exhibit improved physicochemical and pharmacokinetic properties relative to their precursor. This behavior turns these compounds into active reservoirs of Allop, and reduces its unfavorable characteristics, so 2a-f compounds are excellent candidates for the treatment of Chagas disease. This work is therefore an important contribution leading to the suppression of Chagas disease.-
dc.descriptionFil: Gualdesi, María Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina-
dc.descriptionFil: Ortiz, Cristina Susana. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina-
dc.descriptionFil: Raviolo, Mónica Ana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina-
dc.formatapplication/pdf-
dc.formatapplication/pdf-
dc.languageeng-
dc.publisherTaylor-
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.3109/03639045.2015.1061539-
dc.relationinfo:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/full/10.3109/03639045.2015.1061539-
dc.rightsinfo:eu-repo/semantics/restrictedAccess-
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/-
dc.sourcereponame:CONICET Digital (CONICET)-
dc.sourceinstname:Consejo Nacional de Investigaciones Científicas y Técnicas-
dc.sourceinstacron:CONICET-
dc.subjectCHAGAS DISEASE-
dc.subjectN-ACYLOXYMETHYL PRODRUGS-
dc.subjectPHYSICOCHEMICAL AND PHARMACOKINETIC PROPERTIES-
dc.subjectTRYPANOSOMA CRUZI-
dc.subjectTRYPANOSOMAL ACTIVITY-
dc.subjectOtras Ciencias Químicas-
dc.subjectCiencias Químicas-
dc.subjectCIENCIAS NATURALES Y EXACTAS-
dc.titleSynthesis and pharmaceutical properties of N-acyloxymethyl prodrugs of Allop with potential anti-trypanosomal activity-
dc.typeinfo:eu-repo/semantics/article-
dc.typeinfo:eu-repo/semantics/publishedVersion-
dc.typeinfo:ar-repo/semantics/articulo-
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