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Name

Treatment of MSRA infections

Organization name

PROvendis GmbH

Profile

Invention

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.

Commercial Opportunities

On behalf of University of Düsseldorf, PROvendis offers the invention for licensing.

Competitive Advantages

  • High potency
  • Ease of synthetical access

Current Status                                                                                                       

A European priority application has been filed.

Relevant Publication

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

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