Health & Medicine Week
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Antibiotics
N- and C-terminal modifications of negamycin affect antibacterial activity
September 1st, 2003
N- and C-terminal modifications of negamycin affected the drug's antibacterial activity. "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," scientists in the United States report. "The N-terminal modifications have resulted in the identification of active analogues, whereas the C-terminal...
Source: Health & Medicine Week (2003-09-01)
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