Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis

Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)- pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and its corresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)- 2-oxo-5-oxazolidinyl) methyl disodium phosphate (DA-...

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Main Authors: Espinoza González, Nelly Alejandra, Welsh Lozano, Oliverio, De Torres, Noemi Waksman, Cavazos Rocha, Norma Cecilia, Ocampo Candiani, Jorge, Said Fernández, Salvador, Lozano Garza, Gerardo, Choi, Sung Hak, Vera Cabrera, Lucio
Format: Article
Language:English
Published: 2008
Subjects:
Online Access:http://eprints.uanl.mx/15281/1/833.pdf
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author Espinoza González, Nelly Alejandra
Welsh Lozano, Oliverio
De Torres, Noemi Waksman
Cavazos Rocha, Norma Cecilia
Ocampo Candiani, Jorge
Said Fernández, Salvador
Lozano Garza, Gerardo
Choi, Sung Hak
Vera Cabrera, Lucio
author_facet Espinoza González, Nelly Alejandra
Welsh Lozano, Oliverio
De Torres, Noemi Waksman
Cavazos Rocha, Norma Cecilia
Ocampo Candiani, Jorge
Said Fernández, Salvador
Lozano Garza, Gerardo
Choi, Sung Hak
Vera Cabrera, Lucio
author_sort Espinoza González, Nelly Alejandra
collection Repositorio Institucional
description Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)- pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and its corresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)- 2-oxo-5-oxazolidinyl) methyl disodium phosphate (DA-7218), have shown very good activity against several Gram positive bacteria, including Nocardia and Mycobacterium. In the present work we evaluated the therapeutic in vivo effects of DA-7218 on Nocardia brasiliensis. We first determined the plasma concentration of the prodrug in BALB/c mice using several doses and then tested its activity in an in vivo experimental actinomycetoma murine model. At the end of treatment, there was a statistically significant difference between the three drug receiving groups (25, 12.5 and 5 mg/kg) and the control group (saline solution) (p=0.001), proving that DA-7218 is effective for the treatment of experimental murine actinomycetoma. This compound could be a potential option for patients affected with mycetoma by Nocardia brasiliensis.
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spelling eprints-152812024-12-09T17:31:22Z http://eprints.uanl.mx/15281/ Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis Espinoza González, Nelly Alejandra Welsh Lozano, Oliverio De Torres, Noemi Waksman Cavazos Rocha, Norma Cecilia Ocampo Candiani, Jorge Said Fernández, Salvador Lozano Garza, Gerardo Choi, Sung Hak Vera Cabrera, Lucio QR Microbiología Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)- pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and its corresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)- 2-oxo-5-oxazolidinyl) methyl disodium phosphate (DA-7218), have shown very good activity against several Gram positive bacteria, including Nocardia and Mycobacterium. In the present work we evaluated the therapeutic in vivo effects of DA-7218 on Nocardia brasiliensis. We first determined the plasma concentration of the prodrug in BALB/c mice using several doses and then tested its activity in an in vivo experimental actinomycetoma murine model. At the end of treatment, there was a statistically significant difference between the three drug receiving groups (25, 12.5 and 5 mg/kg) and the control group (saline solution) (p=0.001), proving that DA-7218 is effective for the treatment of experimental murine actinomycetoma. This compound could be a potential option for patients affected with mycetoma by Nocardia brasiliensis. 2008 Article PeerReviewed text en cc_by_nc_nd http://eprints.uanl.mx/15281/1/833.pdf http://eprints.uanl.mx/15281/1.haspreviewThumbnailVersion/833.pdf Espinoza González, Nelly Alejandra y Welsh Lozano, Oliverio y De Torres, Noemi Waksman y Cavazos Rocha, Norma Cecilia y Ocampo Candiani, Jorge y Said Fernández, Salvador y Lozano Garza, Gerardo y Choi, Sung Hak y Vera Cabrera, Lucio (2008) Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis. Molecules, 13 (1). pp. 31-40. ISSN 1420-3049 http://doi.org/10.3390/molecules13010031 doi:10.3390/molecules13010031
spellingShingle QR Microbiología
Espinoza González, Nelly Alejandra
Welsh Lozano, Oliverio
De Torres, Noemi Waksman
Cavazos Rocha, Norma Cecilia
Ocampo Candiani, Jorge
Said Fernández, Salvador
Lozano Garza, Gerardo
Choi, Sung Hak
Vera Cabrera, Lucio
Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
thumbnail https://rediab.uanl.mx/themes/sandal5/images/online.png
title Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
title_full Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
title_fullStr Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
title_full_unstemmed Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
title_short Efficacy of DA-7218, a new oxazolidinone prodrug, in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
title_sort efficacy of da 7218 a new oxazolidinone prodrug in the treatment of experimental actinomycetoma produced by nocardia brasiliensis
topic QR Microbiología
url http://eprints.uanl.mx/15281/1/833.pdf
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