Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594367 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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.
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Authors
Sheo B. Singh, Michael A. Goetz, Scott K. Smith, Deborah L. Zink, Jon Polishook, Russell Onishi, Scott Salowe, Judyann Wiltsie, John Allocco, Janet Sigmund, Karen Dorso, Mercedes de la Cruz, Jesús MartÃn, Francisca Vicente, Olga Genilloud,