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National R&D

SEA ANTIMICROBIALS

Pyrazino [1,2-B]Quinazoline-3,6-Diones derivatives, their Production and uses thereof

Principal Investigator
Researcher

Pharmaceutical Chemistry FFUP and Director board member of the Medicinal Chemistry and Biology Division of SPQ. Editor of Bioorganic Chemistry (Elsevier) and Associate Editor of Pharmaceuticals (MDPI).
Area of scientific activity centered on Medicinal Chemistry in particular, in the structure-based design and synthesis of potential drug candidates based on marine natural product leads.
Author of 5 Portuguese and 5 International Patent Applications in the area of drug discovery.

RESEARCH GROUPS:

No results found.

This project aims at the protection of the invention SEA ANTIMICROBIALS through national and international patent.

This invention is based on natural occurring marine natural product fumiquinazolines and fiscalins, described for the first time to be used as antibacterial and antimalarial agents. Among the antibacterial commercially available drugs, bacterial resistance has consecutively emerged as a main medical problem. The derivatives of this invention exhibit activity against methicillin-resistant Staphylococcus aureus (MRSA), inhibiting also the growth of Plasmodium falciparum 3D7. Although they are derived from aminoacids they are non-hemolytic and show potential drug-likeness. They have a simpler structure than the marine product neofiscalin A and contrary to fiscalin C they have intrinsic antibacterial activity and also antimalarial activity. The benefits of this invention include: the production from commercial cheap available building blocks, only one step is required for their synthesis; the synthesis was proven to be suitable for scale-up. Therefore, a formulation containing these compounds as effective components may be used in the treatment of infective diseases. Additionally, these derivatives can be used for example, in disinfection of materials or in cosmetic compositions. The international patent application will represent a competitive advantage in the search for new economic partners to support the developments needed to take Sea Antimicrobials to market and to ensure an effective commercialization, stimulating the national competitiveness.

 

PROJECT SHEET 

Leader Institution
CIIMAR-UP
Program
Portugal 2020
Funding
Other projects