4.5 Article

Identification of novel deoxyribofuranosyl indole antimicrobial agents

Journal

JOURNAL OF ANTIBIOTICS
Volume 65, Issue 2, Pages 53-57

Publisher

JAPAN ANTIBIOTICS RESEARCH ASSOC
DOI: 10.1038/ja.2011.110

Keywords

bactericidal; macromolecule synthesis; MRSA; novel antimicrobial; VRE

Funding

  1. National Institute of Biomedical Innovation (NIBIO)
  2. Grants-in-Aid for Scientific Research [24102510] Funding Source: KAKEN

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Three novel deoxyribofuranosyl indole derivatives, FG050227 (1), FG050223 (2) and FG050204 (3), were identified as antimicrobial agents effective against Gram-positive bacterial strains and some fungi. The MIC values of (1), (2) and (3) against methicillin-resistant Staphylococcus aureus were 3.0, 6.0 and 13 mu gml(-1), respectively. Compounds 1 and 3 had bactericidal activity against exponentially growing S. aureus and inhibited biosynthesis of peptidoglycan, protein, RNA and DNA. Compound 2 was bacteriostatic and inhibited the biosynthesis of protein and RNA. The results indicated that deoxyribofuranosyl indole derivatives could be potential lead compounds for the development of antimicrobial agents. The Journal of Antibiotics (2012) 65, 53-57; doi: 10.1038/ja.2011.110; published online 14 December 2011

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