New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis.

摘要: Abstract A set of structurally diverse N-amino δ-lactams decorated with a 5-nitro-2-furyl moiety was synthesized using isocyanide-based multicomponent chemistry and evaluated for antibacterial activity. Three compounds displayed selective potent (MIC 22-33 μM) inhibition M. tuberculosis H37Rv strain growth, while other Gram-positive (MRSA E. faecium) or Gram-negative (E. coli, P. aeruginosa, A. baumannii, K. pneumoniae) pathogens were not affected. The also moderate-low cytotoxicity, as demonstrated in cell line viability assays. Several multidrug- poly-resistant patient-derived strains found to be susceptible treatment these compounds. three most share significant structural similarity which provides basis further scaffold-hopping analog design.