New Class of inhibitors with activity against Gram-positive and Gram-negative bacteria

Background

The increasing number of life-threatening infections due to resistant Gram-positive and Gram-negative pathogens is alarming. In the last 50 years, the number of multi-drug resistant (MDR) bacteria is rising and the number of drugs crossing the first testing phases is very limited.

Description of invention

We have discovered a new class of inhibitors of the ATPase domains of DNA gyrase and/or topoisomerase IV. The benzothiazole scaffold-based compounds, that can be used in the manufacture of drugs, are effective against both Gram-positive and Gram-negative pathogens in humans. Examples include pathogens of the “ESKAPE” group (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species).

Main advantages

Most inhibitors previously described showed activity only against Gram-positive strains and were not successful in clinical trials due to their high toxicity profile. Our compounds show promising possibilities for derivatization and are active against both Gram-positive and Gram-negative bacteria.