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DIFLUOROBENZYL ETHANOLAMINE DERIVATIVES WITH ANTIMICROBIAL ACTIVITY
WO12013848
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. These diseases cause millions of deaths per year worldwide, making it a priority to find and develop new drugs. A team from the University of Valencia and the Joint UV-Principe Felipe Research Centre have synthesised new compounds with inhibitory activity against the growth of Mycobacterium and Nocardia species. The new compounds obtained belong to the family of fluorinated ethanolamines and have demonstrated, in vitro, a selective antimicrobial activity against the aforementioned microorganisms.
Applications: The main application of the technology is in the pharmaceutical area, as active ingredient for the treatment of infectious diseases caused by Mycobacterium and Nocardia. Advantages: The most remarkable advantages provided by this technology are: - Selectivity of the compounds against species of the genera Mycobacterium and Nocardia. - High in vitro antimicrobial activity, with MIC values similar or lower than those for therapeutic agents in use as ethambutol. - Improvement of pharmacodynamic properties of the potentially active compounds due to the stability provided by the difluorobenzyl group. - Less synthetic steps than existing procedures to obtain the four possible diastereoisomers of the molecules.