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dc.contributor.author
Gualdesi, María Soledad
dc.contributor.author
Ortiz, Cristina Susana
dc.contributor.author
Raviolo, Mónica Ana
dc.date.available
2019-02-04T17:34:29Z
dc.date.issued
2016-01
dc.identifier.citation
Gualdesi, 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.identifier.issn
0363-9045
dc.identifier.uri
http://hdl.handle.net/11336/69296
dc.description.abstract
We 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.format
application/pdf
dc.language.iso
eng
dc.publisher
Taylor
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Chagas Disease
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N-Acyloxymethyl Prodrugs
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Physicochemical And Pharmacokinetic Properties
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Trypanosoma Cruzi
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Trypanosomal Activity
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Otras Ciencias Químicas
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Synthesis and pharmaceutical properties of N-acyloxymethyl prodrugs of Allop with potential anti-trypanosomal activity
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-02-04T13:02:48Z
dc.journal.volume
42
dc.journal.number
4
dc.journal.pagination
602-610
dc.journal.pais
Estados Unidos
dc.journal.ciudad
Nueva York
dc.description.fil
Fil: 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.description.fil
Fil: Ortiz, Cristina Susana. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina
dc.description.fil
Fil: 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.journal.title
Drug Development and Industrial Pharmacy
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://dx.doi.org/10.3109/03639045.2015.1061539
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.tandfonline.com/doi/full/10.3109/03639045.2015.1061539
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