{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,10]],"date-time":"2026-02-10T01:54:20Z","timestamp":1770688460582,"version":"3.49.0"},"reference-count":37,"publisher":"American Society for Microbiology","issue":"8","license":[{"start":{"date-parts":[[2014,8,1]],"date-time":"2014-08-01T00:00:00Z","timestamp":1406851200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2014,8]]},"abstract":"<jats:title>ABSTRACT<\/jats:title><jats:p>We present here the novel ketolide RBx 14255, a semisynthetic macrolide derivative obtained by the derivatization of clarithromycin, for its<jats:italic>in vitro<\/jats:italic>and<jats:italic>in vivo<\/jats:italic>activities against sensitive and macrolide-resistant<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Streptococcus pneumoniae<\/jats:named-content>. RBx 14255 showed excellent<jats:italic>in vitro<\/jats:italic>activity against macrolide-resistant<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>, including an in-house-generated telithromycin-resistant strain (<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>3390 NDDR). RBx 14255 also showed potent protein synthesis inhibition against telithromycin-resistant<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>3390 NDDR. The binding affinity of RBx 14255 toward ribosomes was found to be more than that for other tested drugs. The<jats:italic>in vivo<\/jats:italic>efficacy of RBx 14255 was determined in murine pulmonary infection induced by intranasal inoculation of<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>ATCC 6303 and systemic infection with<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>3390 NDDR strains. The 50% effective dose (ED<jats:sub>50<\/jats:sub>) of RBx 14255 against<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>ATCC 6303 in a murine pulmonary infection model was 3.12 mg\/kg of body weight. In addition, RBx 14255 resulted in 100% survival of mice with systemic infection caused by macrolide-resistant<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. pneumoniae<\/jats:named-content>3390 NDDR at 100 mg\/kg four times daily (QID) and at 50 mg\/kg QID. RBx 14255 showed favorable pharmacokinetic properties that were comparable to those of telithromycin.<\/jats:p>","DOI":"10.1128\/aac.01589-13","type":"journal-article","created":{"date-parts":[[2014,2,19]],"date-time":"2014-02-19T05:16:41Z","timestamp":1392787001000},"page":"4283-4289","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":5,"title":["A Novel Ketolide, RBx 14255, with Activity against Multidrug-Resistant Streptococcus pneumoniae"],"prefix":"10.1128","volume":"58","author":[{"given":"V. 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