Sulfonamide-based non-alkyne LpxC inhibitors as Gram-negative antibacterial agents.

We attempted to optimize sulfonamide-based non-alkyne LpxC inhibitors by focusing on improvements in enzyme inhibitory and antibacterial activity. It was discovered that inhibitors possessing 2-aryl benzofuran as a hydrophobe exhibited good activity. In particular, compound 21 displayed impressive antibacterial activity (E. coli MIC=0.063µg/mL, K. pneumoniae MIC=0.5µg/mL, and P. aeruginosa MIC=0.5µg/mL), and is a promising lead for further exploration as an antibacterial agent.