Breaking a vicious circle: the search for novel antimicrobial agents

Since the introduction of antimicrobial agents, micro-organisms have developed numerous defences rendering them resistant to these drugs. Antimicrobial resistance, in particular multi-drug resistance, is increasing at an alarming rate and severely compromises our ability to deal with infectious diseases. Over the last three decades, numerous efforts have been devoted to the research  and development of generations of new antibiotic drugs. A team of researchers involved in organic synthesis managed by Dr Jean-Noël DENIS at the Molecular Chemistry Department of Grenoble who contributed to the development of Taxotere and taxol, the anticancer blockbusters, has recently discovered a novel family of indole derivatives revealing significant potential as antimicrobial agents, particularly with regards to their resistance-reversing effects. The development of these molecules as new drug candidates has recently been funded by the National Research Agency (l'Agence Nationale de la Recherche).

Key Benefits

• An original synthesis pathway allowing access to a wide range of derivatives
• Interesting growth inhibition effects on sensitive bacterial strains of Staphylococcus aureus
• Demonstrated resistance-reversing activity towards resistant strains of Staphylococcus aureus (NorA strain)
• Low cytotoxicity on human cell lines
• The know-how and expertise to work out mechanisms of action and enhance activity of ideal candidates

Intellectual Property

The synthesis pathway and the antimicrobial properties of these indole derivatives are protected by a European Patent.

Potential Applications

• Antibacterial and Antifungal drug development

When subjected to resistant strains of bacteria over expressing antibiotic efflux pumps, some of the tested indole derivatives were observed to totally restore the sensitivity of the bacteria to the widely used antibiotic ciprofloxacin.

Floralis is currently looking for industrial partners interested in further developing this exciting technology.

Contacts

Mathieu TILQUIN
Technology Transfer
+33 (0)4 76 00 78 41
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