{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T03:55:45Z","timestamp":1790913345935,"version":"4.1.0"},"reference-count":18,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2008,1,11]],"date-time":"2008-01-11T00:00:00Z","timestamp":1200009600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>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.<\/jats:p>","DOI":"10.3390\/molecules13010031","type":"journal-article","created":{"date-parts":[[2008,10,2]],"date-time":"2008-10-02T12:45:09Z","timestamp":1222951509000},"page":"31-40","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":20,"title":["Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis"],"prefix":"10.3390","volume":"13","author":[{"given":"Nelly Alejandra","family":"Espinoza-Gonz\u00e1lez","sequence":"first","affiliation":[{"name":"Servicio de Dermatolog\u00eda, Hospital Universitario \u201cDr. Jos\u00e9 E. Gonz\u00e1lez\u201d Ave. Madero y Gonzalitos S\/N Col. Mitras Centro Monterrey, N.L. M\u00e9xico 64460"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Oliverio","family":"Welsh","sequence":"additional","affiliation":[{"name":"Servicio de Dermatolog\u00eda, Hospital Universitario \u201cDr. Jos\u00e9 E. Gonz\u00e1lez\u201d Ave. Madero y Gonzalitos S\/N Col. Mitras Centro Monterrey, N.L. M\u00e9xico 64460"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Noemi Waksman","family":"De Torres","sequence":"additional","affiliation":[{"name":"Departamento de Qu\u00edmica Anal\u00edtica, Facultad de Medicina, Universidad Aut\u00f3noma de Nuevo Le\u00f3n, San Nicol\u00e1s de los Garza, Nuevo Le\u00f3n, Mexico"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Norma","family":"Cavazos-Rocha","sequence":"additional","affiliation":[{"name":"Departamento de Qu\u00edmica Anal\u00edtica, Facultad de Medicina, Universidad Aut\u00f3noma de Nuevo Le\u00f3n, San Nicol\u00e1s de los Garza, Nuevo Le\u00f3n, Mexico"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jorge","family":"Ocampo-Candiani","sequence":"additional","affiliation":[{"name":"Servicio de Dermatolog\u00eda, Hospital Universitario \u201cDr. Jos\u00e9 E. Gonz\u00e1lez\u201d Ave. Madero y Gonzalitos S\/N Col. Mitras Centro Monterrey, N.L. M\u00e9xico 64460"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Salvador","family":"Said-Fernandez","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica del Noreste (CIBIN) del IMSS, 2 de Abril y San Luis Potos\u00ed, Col. Independencia, Monterrey, N.L., M\u00e9xico 64720"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gerardo","family":"Lozano-Garza","sequence":"additional","affiliation":[{"name":"Centro de Investigaci\u00f3n Biom\u00e9dica del Noreste (CIBIN) del IMSS, 2 de Abril y San Luis Potos\u00ed, Col. Independencia, Monterrey, N.L., M\u00e9xico 64720"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sung-Hak","family":"Choi","sequence":"additional","affiliation":[{"name":"Research Laboratory, Dong-A Pharmaceutical Co., Ltd., Yongin, and College of Pharmacy, Sungkyunkwan University, Suwon, South Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lucio","family":"Vera-Cabrera","sequence":"additional","affiliation":[{"name":"Servicio de Dermatolog\u00eda, Hospital Universitario \u201cDr. Jos\u00e9 E. Gonz\u00e1lez\u201d Ave. Madero y Gonzalitos S\/N Col. Mitras Centro Monterrey, N.L. M\u00e9xico 64460"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2008,1,11]]},"reference":[{"key":"ref_1","first-page":"435","article-title":"Oxazolidinones: A new Class of Antimicrobials","volume":"16","author":"Ford","year":"1999","journal-title":"Infect. Med."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"7","DOI":"10.2165\/00003495-200059010-00002","article-title":"Oxazolidinones: a review","volume":"59","author":"Diekema","year":"2000","journal-title":"Drugs"},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"955","DOI":"10.1211\/jpp.59.7.0007","article-title":"Pharmacokinetics of DA-7218, a new oxazolidinone, and its active metabolite, DA-7157, after intravenous and oral administration of DA-7218 and DA-7157 to rats","volume":"59","author":"Bae","year":"2007","journal-title":"J. Pharm. Pharmacol."},{"key":"ref_4","first-page":"477","article-title":"Epidemiolog\u00eda del micetoma en M\u00e9xico: estudio de 2105 casos","volume":"128","author":"Lavalle","year":"1992","journal-title":"Gac. Med. Mex."},{"key":"ref_5","doi-asserted-by":"crossref","first-page":"308","DOI":"10.1111\/j.1365-2133.2006.07557.x","article-title":"Treatment of actinomycetoma due to Nocardia spp. with amoxicillin-clavulanate","volume":"156","author":"Bonifaz","year":"2007","journal-title":"Br. J. Dermatol."},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"50-2","DOI":"10.1097\/01.inf.0000247108.86199.64","article-title":"Mycetoma in children: experience with 15 cases","volume":"26","author":"Bonifaz","year":"2007","journal-title":"Pediatr. Infect. Dis. J."},{"key":"ref_7","first-page":"247","article-title":"Actinomycetoma and Nocardia sp. Report of five cases treated with imipenem or imipenem plus amikacin","volume":"142","author":"Fuentes","year":"2006","journal-title":"Gac. Med. Mex."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"387","DOI":"10.1111\/j.1365-4362.1991.tb03892.x","article-title":"Mycetoma. Current concepts in treatment","volume":"30","author":"Welsh","year":"1991","journal-title":"Int. J. Dermatol."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"195","DOI":"10.1016\/j.clindermatol.2006.05.011","article-title":"Mycetoma","volume":"25","author":"Welsh","year":"2007","journal-title":"Clin. Dermatol."},{"key":"ref_10","unstructured":"Welsh, O., and Vera-Cabrera, L. (2003, January May). Abstr. 15th Cong. Int. Soc. Human and Anim. Micol., San Antonio, TX, USA. abstr. 354."},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"3170","DOI":"10.1128\/AAC.00571-06","article-title":"In vitro activities of DA-7157 and DA-7218 against Mycobacterium tuberculosis and Nocardia brasiliensis","volume":"50","author":"Gonzalez","year":"2006","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref_12","first-page":"773","article-title":"Producci\u00f3n experimental del micetoma por Nocardia brasiliensis en el rat\u00f3n","volume":"99","year":"1969","journal-title":"Gac. Med. Mex."},{"key":"ref_13","first-page":"183","article-title":"Experimental mycetoma by Nocardia brasiliensis in rats","volume":"8","author":"Boiron","year":"1998","journal-title":"J. Mycol. Med."},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"3789","DOI":"10.1128\/AAC.47.12.3789-3794.2003","article-title":"Concentrations in plasma, urinary excretion, and bactericidal activity of linezolid (600 milligrams) versus those of ciprofloxacin (500 milligrams) in healthy volunteers receiving a single oral dose","volume":"47","author":"Wagenlehner","year":"2003","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"313","DOI":"10.1086\/345907","article-title":"Clinical experience with linezolid for the treatment of nocardia infection","volume":"36","author":"Moylett","year":"2003","journal-title":"Clin. Infect. Dis."},{"key":"ref_16","doi-asserted-by":"crossref","first-page":"1694","DOI":"10.1345\/aph.1K196","article-title":"Linezolid for the treatment of Nocardia spp. infections","volume":"41","author":"Jodlowski","year":"2007","journal-title":"Ann. Pharmacother."},{"key":"ref_17","unstructured":"Lee, K., Yum, J. H., Yong, D., Chong, Y., Choi, S. H., and Rhee, J. K. (2,, January October). Comparative in vitro activity of DA-70157, a novel oxazolidinone, against recent clinical isolates of aerobic and anaerobic bacteria. 44th Intersci. Conf. Antimicrob. Agents Chemother., Washington, DC, USA. abstr. F1419."},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"832","DOI":"10.1128\/AAC.48.3.832-837.2004","article-title":"In vitro and in vivo activities of antimicrobials against Nocardia brasiliensis","volume":"48","author":"Welsh","year":"2004","journal-title":"Antimicrob. Agents Chemother."}],"container-title":["Molecules"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1420-3049\/13\/1\/31\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T22:20:22Z","timestamp":1760221222000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1420-3049\/13\/1\/31"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2008,1,11]]},"references-count":18,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2008,1]]}},"alternative-id":["13010031"],"URL":"https:\/\/doi.org\/10.3390\/molecules13010031","relation":{},"ISSN":["1420-3049"],"issn-type":[{"value":"1420-3049","type":"electronic"}],"subject":[],"published":{"date-parts":[[2008,1,11]]}}}