Molecules 2008, 13(1), 31-40; doi:10.3390/molecules13010031
Article

Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis

1 Servicio de Dermatología, Hospital Universitario “Dr. José E. González” Ave. Madero y Gonzalitos S/N Col. Mitras Centro Monterrey, N.L. México 64460 2 Departamento de Química Analítica, Facultad de Medicina, Universidad Autónoma de Nuevo León, San Nicolás de los Garza, Nuevo León, Mexico 3 Centro de Investigación Biomédica del Noreste (CIBIN) del IMSS, 2 de Abril y San Luis Potosí, Col. Independencia, Monterrey, N.L., México 64720 4 Research Laboratory, Dong-A Pharmaceutical Co., Ltd., Yongin, and College of Pharmacy, Sungkyunkwan University, Suwon, South Korea
* Author to whom correspondence should be addressed.
Received: 2 November 2007; in revised form: 29 December 2007 / Accepted: 29 December 2007 / Published: 11 January 2008
(This article belongs to the Special Issue Prodrugs)
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Abstract: Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and itscorresponding 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 goodactivity against several Gram positive bacteria, including Nocardia and Mycobacterium. Inthe present work we evaluated the therapeutic in vivo effects of DA-7218 on Nocardiabrasiliensis. We first determined the plasma concentration of the prodrug in BALB/c miceusing several doses and then tested its activity in an in vivo experimental actinomycetomamurine model. At the end of treatment, there was a statistically significant differencebetween 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 forpatients affected with mycetoma by Nocardia brasiliensis.
Keywords: actinomycetoma; oxazolidinones; prodrug; Nocardia brasiliensis

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MDPI and ACS Style

Espinoza-González, N.A.; Welsh, O.; De Torres, N.W.; Cavazos-Rocha, N.; Ocampo-Candiani, J.; Said-Fernandez, S.; Lozano-Garza, G.; Choi, S.-H.; Vera-Cabrera, L. Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis. Molecules 2008, 13, 31-40.

AMA Style

Espinoza-González NA, Welsh O, De Torres NW, Cavazos-Rocha N, Ocampo-Candiani J, Said-Fernandez S, Lozano-Garza G, Choi S-H, Vera-Cabrera L. Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis. Molecules. 2008; 13(1):31-40.

Chicago/Turabian Style

Espinoza-González, Nelly A.; Welsh, Oliverio; De Torres, Noemi W.; Cavazos-Rocha, Norma; Ocampo-Candiani, Jorge; Said-Fernandez, Salvador; Lozano-Garza, Gerardo; Choi, Sung-Hak; Vera-Cabrera, Lucio. 2008. "Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis." Molecules 13, no. 1: 31-40.

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