By employing synthetic combinatorial libraries, our inventors have synthesized a class of bis-cyclic guanidine compounds that were found to have anti-bacterial activity against all six ESKAPE human pathogens. These compounds show promising efficacy in combating bacterial infections, while showing limited toxicity to human cells. The compounds exhibit potent anti-biofilm properties as well.
Front runner bis-cyclic guanidines (red, blue, and green), are efficacious during in vivo infection. Mice were infected with a lethal dose of S. aureus and treated 1h post infection.