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Bioorg Med Chem Lett. 2012 Dec 1;22(23):7127-30. doi: 10.1016/j.bmcl.2012.09.071. Epub 2012 Oct 2.

Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.

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Infectious Diseases, Merck Research Laboratories, Merck & Co., PO Box 2000, Rahway, NJ 07065, USA.


Emergence of bacterial resistance has eroded the effectiveness of many life saving antibiotics leading to an urgent need for new chemical classes of antibacterial agents. We have applied a Staphylococcus aureus fitness test strategy to natural products screening to meet this challenge. In this paper we report the discovery of kibdelomycin A, a demethylated congener of kibdelomycin, the representative of a novel class of antibiotics produced by a new strain of Kibdelosporangium. Kibdelomycin A is a potent inhibitor of DNA gyrase and topoisomerase IV, inhibits DNA synthesis and shows whole cell antibiotic activity, albeit, less potently than kibdelomycin. Kibdelomycin C-33 acetate and tetrahydro-bisdechloro derivatives of kibdelomycin were prepared which helped define a basic SAR of the family.

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