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Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis
Servicio de Dermatología, Hospital Universitario “Dr. José E. González” Ave. Madero y Gonzalitos S/N Col. Mitras Centro Monterrey, N.L. México 64460
Departamento de Química Analítica, Facultad de Medicina, Universidad Autónoma de Nuevo León, San Nicolás de los Garza, Nuevo León, Mexico
Centro de Investigación Biomédica del Noreste (CIBIN) del IMSS, 2 de Abril y San Luis Potosí, Col. Independencia, Monterrey, N.L., México 64720
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
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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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.
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.
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.