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Nueva clase de antibióticos

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TODE20180412001
Publicado:
25/04/2018
Caducidad:
26/04/2019
Resumen:
Una universidad alemana ha desarrollado una nueva clase de antibióticos que se encuentran en fase muy temprana de desarrollo. Específicamente ha preparado y caracterizado una serie de nuevos complejos de carbeno Re(I)-(CO)3-N-heterocíclico que soportan ligandos de benzimidazol-2-ilideno no sustituidos, así como una variedad de ligandos de bis(imino). Los complejos presentan una potente actividad antimicrobiana contra cepas bacterianas Gram-positivas en concentraciones micromoleculares bajas. La universidad busca compañías farmacéuticas especializadas en antibióticos con el fin de establecer acuerdos de licencia.

Details

Tittle:
Novel antibiotic drug class.
Summary:
A German university has developed a new drug class for antibiotics against bacteria. The invention is still at a very early stage. The university offers a license agreement. This technology offer addresses pharmaceutical companies specialized in antibiotics.
Description:
Antibiotic resistance is increasingly becoming an issue when we hear about the treatment of various diseases. A German university developed a new drug class that might lead to novel antibiotics against bacteria.


A series of novel Re(I)-(CO)3-N-heterocyclic carbene (NHC) complexes that bear unsubstituted benzimidazol-2-ylidene ligands as well as a variety of bisimine ligands have been prepared and comprehensively characterised. The complexes were found to exhibit potent antimicrobial activity against Gram-positive bacterial strains in the low micromolar concentration range. Thus they render these compounds into interesting lead structures for the development of novel metal-based antibiotic agents.

Technical details regarding anti-Gram-positive activity:
Substances have good activity against bacillus subtilis and staphylococcus aureus. Activity against methicillin-resistant staphylococcus aureus (MRSA) strains were in the low and sub-micromolar range. No anti-Gram-negative activity was observed.
Elongation factor thermo unstable (EF-Tu) was identified as target in pull-down experiments using biotinylated compound. Protein biosynthesis inhibition was detected in precursor incorporation experiments using unlabeled compound.

Validated target:
Protein biosynthesis inhibition was observed and EF-Tu identified as target protein. Protein biosynthesis is a clinically validated target. Comparative proteomics studies suggest that the mechanism of action is different from known EF-Tu inhibitors.

The university offers a license agreement to pharmaceutical companies specialized in antibiotics. The invention is at a very early stage. Preclinical research still needs to be done.
Advantages and Innovations:
This invention represents a completely novel antibiotic class. Other advantages are:
- Activity against Gram-positive bacteria
- Inhibits translation - a validated target
Stage of Development:
Under development/lab tested
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
A German patent has been filed.

Partner sought

Type and Role of Partner Sought:
The university offers a license agreement to pharmaceutical companies specialized in antibiotics. The invention is at a very early stage. Preclinical research, pharmacodynamics and pharmacokinetics, as well as the whole clinical phase still need to be done.

Client

Type and Size of Client:
University
Already Engaged in Trans-National Cooperation:
Si
Languages Spoken:
English
German

Keywords

Technology Keywords:
06001002 Investigaciones clínicas, ensayos
06001012 Investigaciones médicas
06001015 Productos farmacéuticos / medicamentos
06001018 Virus, virología / antibióticos / bacteriología