• Universitat de València

Pathogenic bacteria of the genera Mycobacterium and Nocardia are implicated in diseases such as tuberculosis, leprosy and other infections of the lung, skin and central nervous system. In particular, Mycobacterium tuberculosis (TB) is the cause of human tuberculosis and is responsible for almost two million deaths per year worldwide, and is one of the most common opportunistic pathogens in HIV+ patients. Several compounds are currently active against TB, such as isoniazid and pyrazinamide, which affect the bacterium's synthesis of fatty acids, and ethambutol, which is involved in the biosynthesis processes of the bacterium's cell wall. However, it is a priority to find and develop new drugs that shorten the duration of existing treatments and solve the resistance problems of the drugs in use.

Researchers from the Universitat de València and the Príncipe Felipe Research Centre have synthesised new compounds with growth inhibitory activity against Mycobacterium and Nocardia species. The new compounds obtained belong to the family of fluorinated ethanolamines, specifically difluorobenzyl ethanolamines, and have demonstrated in vitro a selective antimicrobial activity against the aforementioned microorganisms. This selectivity suggests a specific mechanism of action on special characteristics of these species. In addition, the synthesised molecules show minimum inhibitory concentration (MIC) values similar to or lower than those of a first-line antituberculosis agent such as ethambutol, currently used in the treatment of various forms of tuberculosis.

The main application of the technology is in the pharmaceutical sector, as an active ingredient for the treatment of infectious diseases caused by Mycobacterium and Nocardia.

The main advantages provided by the invention are:

• Selectivity of the molecules against species of the genera Mycobacterium and Nocardia.
• Potent in vitro antimicrobial activity, with MIC values similar or lower than those of therapeutic agents in use such as ethambutol.
• Improved pharmacodynamics of potentially active compounds, due to the stability provided by diflluorobenzyl grouping.
• Fewer synthetic steps in the process of obtaining the four possible diastereoisomers of the molecules.

• Patent granted