Life Sciences

Life Sciences

Compounds activating the glmS riboswitch - Cyclohexane compounds and their use as antibiotics



Ref.-Nr. 2728

The present invention relates to cyclohexane compounds for the treatment of a bacterial infection, particularly for use as an antibiotic. Since the discovery of antibiotic substances and their use against microbes, bacteria have evolved to defend themselves by acquiring resistances. Especially in hospitals where bacteria are exposed to a wide array of antibacterial substances, multiresistant strains (e.g. MRSA) arose.

This is why it is not only necessary to have an ongoing search for new antibiotic substances, but to also find and use new antibacterial targets enforcing new mechanisms of action.

Riboswitches have appeared as one new promising target for antibacterial defence. Riboswitches are mostly found in the 5'-untranslated region of bacterial mRNA and regulate 2-4% of all bacterial genes. In the past it has been shown that metabolite analogues can be employed to trigger riboswitch function thereby modulating its regulatory character. Thus, it would be desirable to provide compounds that also target the glmS riboswitch and exhibit antimicrobial activity.

Keywords: Antibiotika, Antiinfektiva, Glms riboswitch, Cyclohexane compounds, Cyclohexanderivate, antibiotics, antiinfectives

The problem is solved by compounds according to general formula (I) as shown in the figure above. Detailed in vitro characterisation of compounds is already done as well as first in vivo tests on Staphylococcus aureus.

Next planned steps are more substantial in vivo tests, especially with Vancomycin-resistent S. aureus strains.

Beneficially, the compounds according to the invention can be useful as an antibacterial substance in the treatment of bacterial infection. The present invention therefore provides a novel approach to the treatment of bacterial infection.

Commercial Opportunities

On behalf of the Universities of Bonn and Konstanz, PROvendis is offering access for commercial use in terms of a license as well as research collaboration to innovative companies.

Current Status

A European and a US-patent application have been filed.

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