Marine compounds with antimicrobial Activity

Infectious diseases caused by microorganisms stand as a major threat to public health. In particular, antibacterial resistance has increased dramatically, becoming an emergency in healthcare. Likewise, malaria represents a major threat to the public health worldwide. The need to identify new chemical diversity is emergent, ideally with novel modes of action.

The invention describes the synthesis and the use of synthetic pyrazino [1,2-b]quinazoline-3,6-diones derivatives, a new class of compounds with antibacterial and/or antimalarial activities. The compounds are a subclass of alkaloids mostly isolated from marine and terrestrial sources. Best lead compounds are potent antimicrobials against methicillin-resistant Staphylococcus aureus (MIC 4-8 μg/mL) and others against Plasmodium falciparum 3D7 (IC50 0.02-2 μg/mL). Molecular docking studies support the inhibition of gene expression of Plasmodium and Leishmania sp. via prolyl-tRNA synthetase.

Advantages:
• Unique chemical structure with one-step synthesis from cheap building blocks;
• Potent antimicrobial activity against multi-resistant bacterial pathogens and antimalarial activity;
• Compounds had no hemolytic nor cytotoxic effects at MIC/IC50 concentrations.

Current development status

Experimental technologies

Applications

Pharmaceutical; Treatment of bacterial infections; Treatment of malaria; Antibacterial coatings and surfaces.

Desired business relationship

Technology selling

Patent licensing

Technology development