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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.

Author information

1
Infectious Diseases, Merck Research Laboratories, Merck & Co., PO Box 2000, Rahway, NJ 07065, USA. sheo_singh@merck.com

Abstract

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.

PMID:
23084277
DOI:
10.1016/j.bmcl.2012.09.071
[Indexed for MEDLINE]

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