title: Synthesis and antibacterial activity of novel 4-aryl-[1,2,3]-triazole containing macrolides.
abstract: Two series of novel triazole containing 14-member macrolides having either a cladinose or a 3-pyridyl acetate group at the 3-position of the macrolide ring were synthesized. The in vitro antibacterial activities against S. aureus, S. pneumoniae, S. pyogenes and E. faecalis were determined. Macrolide 7a and the fluoroketolide 1 (CEM-101) were evaluated in vivo in murine systemic infection models. All of the macrolide analogs were less active in vitro and in vivo than the fluoroketolide 1 (CEM-101).
authors.affiliation: Cempra Pharmaceuticals, Inc, Building Four Quadrangle, 6340 Quadrangle Drive, Suite 100, Chapel Hill, NC 27517, United States. dpereira@cempra.com
authors.forename: David
authors.initials: D
authors.lastname: Pereira
authors.forename: Prabhavathi
authors.initials: P
authors.lastname: Fernandes
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016470:Bacteremia / Q000188:drug therapy; D018942:Macrolides / Q000737:chemistry*; D051379:Mice; D008826:Microbial Sensitivity Tests; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D018942:Macrolides; D014230:Triazoles