negamycin and Sepsis

negamycin has been researched along with Sepsis* in 1 studies

Other Studies

1 other study(ies) available for negamycin and Sepsis

Article	Year
N- and C-terminal modifications of negamycin. Bioorganic & medicinal chemistry letters, 2003, Jul-21, Volume: 13, Issue:14 Negamycin 1 is a bactericidal antibiotic with activity against Gram-negative bacteria, and served as a template in an antibiotic discovery program. An orthogonally protected beta-amino acid derivative 3a was synthesized and used in parallel synthesis of negamycin derivatives on solid support. This advanced intermediate was also used for N- and C-terminal modifications using solution-phase methodologies. The N-terminal modifications have resulted in the identification of active analogues, whereas the C-terminal modifications resulted in complete loss of antibacterial activity. The N-methyl negamycin analogue, 19a, inhibits protein synthesis (IC(50)=2.3 microM), has antibacterial activity (Escherichia coli, MIC=16 microgram/mL), and is efficacious in an E. coli murine septicemia model (ED(50)=16.3mg/kg). Topics: Amino Acids, Diamino; Animals; Anti-Bacterial Agents; Bacteria; Bacterial Proteins; Drug Design; Escherichia coli; Escherichia coli Infections; Hydrazines; Indicators and Reagents; Mice; Microbial Sensitivity Tests; Molecular Conformation; Protein Synthesis Inhibitors; Sepsis	2003

Article

Year

N- and C-terminal modifications of negamycin.

Bioorganic & medicinal chemistry letters, 2003, Jul-21, Volume: 13, Issue:14

Negamycin 1 is a bactericidal antibiotic with activity against Gram-negative bacteria, and served as a template in an antibiotic discovery program. An orthogonally protected beta-amino acid derivative 3a was synthesized and used in parallel synthesis of negamycin derivatives on solid support. This advanced intermediate was also used for N- and C-terminal modifications using solution-phase methodologies. The N-terminal modifications have resulted in the identification of active analogues, whereas the C-terminal modifications resulted in complete loss of antibacterial activity. The N-methyl negamycin analogue, 19a, inhibits protein synthesis (IC(50)=2.3 microM), has antibacterial activity (Escherichia coli, MIC=16 microgram/mL), and is efficacious in an E. coli murine septicemia model (ED(50)=16.3mg/kg).

Topics: Amino Acids, Diamino; Animals; Anti-Bacterial Agents; Bacteria; Bacterial Proteins; Drug Design; Escherichia coli; Escherichia coli Infections; Hydrazines; Indicators and Reagents; Mice; Microbial Sensitivity Tests; Molecular Conformation; Protein Synthesis Inhibitors; Sepsis

2003