Rational N-Terminal Tuning of Bacitracin A: Repurposing a Classic Antibiotic to Combat Multidrug-Resistant Gram-Positive Pathogens.
A site-selective semisynthetic modification strategy via reductive amination of bacitracin A's N-terminal primary amine is established, providing a rational strategy for bacitracin optimization and highlighting the potential of N-terminal modification for developing improved antibacterial agents.