Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics |
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| Authors: | Henninger Todd C Xu Xiaodong Abbanat Darren Baum Ellen Z Foleno Barbara D Hilliard Jamese J Bush Karen Hlasta Dennis J Macielag Mark J |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. thenning@prdus.jnj.com |
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| Abstract: | A new series of antibacterial ketolides is reported, which features the use of a C-6 carbamate for tethering the arylalkyl sidechain to the macrolide core. The best members of this series display in vitro and in vivo activity comparable to telithromycin. Partial epimerization at C-2, unobserved in previously reported ketolides, was noted for this series. |
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