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Bioorg Med Chem Lett. 2011 Jan 1;21(1):510-3. doi: 10.1016/j.bmcl.2010.10.091. Epub 2010 Oct 25.

Synthesis and antibacterial activity of novel 4-aryl-[1,2,3]-triazole containing macrolides.

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  • 1Cempra Pharmaceuticals, Inc, Building Four Quadrangle, 6340 Quadrangle Drive, Suite 100, Chapel Hill, NC 27517, United States.


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).

Copyright © 2010 Elsevier Ltd. All rights reserved.

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