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Kibdelomycin A, a congener of kibdelomycin, derivatives and their antibacterial activities.
Singh, Sheo B; Goetz, Michael A; Smith, Scott K; Zink, Deborah L; Polishook, Jon; Onishi, Russell; Salowe, Scott; Wiltsie, Judyann; Allocco, John; Sigmund, Janet; Dorso, Karen; de la Cruz, Mercedes; Martín, Jesús; Vicente, Francisca; Genilloud, Olga; Donald, Robert G K; Phillips, John W.
Afiliação
  • Singh SB; Infectious Diseases, Merck Research Laboratories, Merck & Co., PO Box 2000, Rahway, NJ 07065, USA. sheo_singh@merck.com
Bioorg Med Chem Lett ; 22(23): 7127-30, 2012 Dec 01.
Article em En | MEDLINE | ID: mdl-23084277
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.
Assuntos

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Aminoglicosídeos / Antibacterianos / Naftalenos Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2012 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Aminoglicosídeos / Antibacterianos / Naftalenos Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2012 Tipo de documento: Article País de afiliação: Estados Unidos