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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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