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COMPOUNDS ACTIVE ON INFECTED HOST CELLS

Anti-bacterial activityanti-fungalantinfective agentsbenzo-carbazole compoundshost cell

Introduction

The invention relates to the use of compounds of benzo[a]carbazole structure of formula (I) in the prevention and/or treatment of infectious diseases caused by pathogenic organisms. The compounds act directly on the infected cells of the patient. According to the invention, these compounds do not exhibit direct antibacterial activity when tested on bacterial cultures. They do not act on the infecting agent, but rather on the infected cells of the host and therefore should not produce those treatment resistance effects typical of various classes of antibacterial, antiviral, antifungal and antiprotozoal agents.

Technical features

Our patented molecules (I) are capable, through a mechanism common to different types of infection (e.g., bacterial, fungal, viral, or due to protozoa), of blocking infection in the patient not by acting directly on the pathogen but by reactivating a protective mechanism in the host cells based on increasing the levels of p53 protein, which plays a key role in the intracellular development of the pathogen. Here we demonstrated the ability of our type (I) compounds to block Chlamydia trachomatis infection in host cells through a mechanism that does not act directly on the pathogen. In fact, these compounds do not exhibit direct antibacterial activity when tested on bacterial cultures (e.g., Staphylococcus aureus). These results can be translated to other pathogens that use the same oncogenic mechanism involving the reduction of intracellular p53 protein levels to protect infected cells from apoptosis. Thus these compounds, acting through this common mechanism, could simultaneously target several pathogens including bacteria, fungi, viruses, and protozoa.

Possible Applications

  • Blocking infection in the patient;
  • Use in combination with other drug classes in infections caused by pathogens of various types;
  • Use for marking infected cells and tissues for diagnostic purposes.

Advantages

  • Action not directly related to the biological functions of the infectious agent;
  • Considerable reduction in the risk of selection, mutation, and resistance due to the use of common drugs;
  • Reduction in therapeutic risk due to commonly used drugs.