Treatment of MSRA infections
Infection with methicillin-resistant Staphylococcus aureus (MRSA) is a major health problem in hospitals, long-term care facilities, and community medicine settings worldwide. There are new compounds in development for the treatment of MRSA. Unfortunately, there is a significant risk that new antibiotics targeting pathogen-specific proteins will exert the sort of selective pressure on the pathogen that ultimately leads to antibiotic resistance. Consequently, there is still a medical need for new antibiotics targeting MRSA.
The inventors of the present invention identified derivatives of the bis-indol-compounds hyrtinadine A and allocasine A as being active against MRSA. The minimum inhibitory concentration of compounds is in the sub-micromolar range. The strong bactericidal effect seems to suppress the formation of any resistances.
Next to its potency, easy synthetical access is a key feature of the compounds of the present invention. The compounds are accessible by a one-pot synthesis. The molecular scaffold may easily be modified in order to develop further derivatives.
On behalf of University of Düsseldorf, PROvendis offers the invention for licensing.
- High potency
- Ease of synthetical access
A European priority application has been filed.
Tasch, B.O. et al. (2013) Masuda borylation-Suzuki coupling (MBSC) sequence of vinylhalides and its application in a one-pot synthesis of 3,4-biarylpyrazoles. Org.Biomol. Chem. 11(36): 6113-8