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Ruta de síntesis total para la producción de albicidina a escala de multigramos

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TODE20191106001
Publicado:
13/11/2019
Caducidad:
13/11/2020
Resumen:
Una universidad alemana ha desarrollado una ruta de síntesis convergente de albicidina que permite la producción a escala de multigramos de antibiótico y, como consecuencia, el perfilado de las propiedades del medicamento. Dentro de esta ruta de síntesis se han identificado varios bloques de construcción que pueden sintetizarse de forma separada. Las modificaciones dentro de estos bloques permiten la producción de varios derivados con diferentes propiedades. Las variaciones en los bloques de construcción de albicidina ofrecen compuestos con propiedades antibióticas relevantes, en particular actividad antibiótica contra patógenos resistentes. La universidad busca socios con el fin de establecer un acuerdo de cooperación en materia de investigación o licencia.

Details

Tittle:
Total synthesis route enabling the production in multi gram amounts of albicidin
Summary:
A Berlin-based German university has developed a convergent synthesis route towards albicidin. This enables the production of multi gram amounts of the antibiotic substance and, as a consequence, the further profiling of its drug properties. They are interested in the further development of the technology in the framework of a research cooperation or a license agreement.
Description:
Due to the increasing development of antibiotic resistances by bacterial pathogens, there is a tremendous need for the development of new antibiotic lead structures. Major causes of concern are hereby Gram-negative bacteria as infections with those bacteria are very difficult to treat.

Gram-negative bacteria are a group of bacteria that do not retain the crystal violet stain used in the Gram staining method of bacterial differentiation. They are characterized by their cell envelopes, which are composed of a thin peptidoglycan cell wall sandwiched between an inner cytoplasmic cell membrane and a bacterial outer membrane. Gram-negative bacteria are spread worldwide, in virtually all environments that support life. The gram-negative bacteria include the model organism Escherichia coli, as well as many pathogenic bacteria.

Thus there is a high need to identify and develop new antibiotics that are highly effective and can overcome current resistances.
Albicidin has the potential to be such a compound as it displays remarkable antibacterial activity against various Gram-positive and Gram-negative microorganisms. Initially described as an antibiotic and phytotoxic substance derived by the plant pathogenic bacterium Xanthomonas albilineans in 1985 its molecular structure was determined only recently. Currently, limiting factors in providing sufficient material for therapeutic usage are the only low amounts of albicidin obtainable.

Scientists at a Berlin-based German university now developed a convergent total synthesis route toward albicidin enabling the production in multi gram amounts of albicidin that can be used for further profiling of its drug properties. Within this synthesis route various building blocks were identified that can be synthesized separately. Modifications within these building blocks enable the production of several derivatives with different properties.

Those variations in the building blocks of albicidin can provide compounds with relevant antibiotic properties, in particular an antibiotic activity against resistant pathogens.

The university is interested in a cooperation in the framework of a license agreement or a research cooperation agreement. A future licensee would have the authorization to use the synthesis route in return for a fee or a share of royalties. They would also agree to a research cooperation agreement which leads to further profiling of the drug properties of albicidin.
Advantages and Innovations:
· First total synthesis route to the novel antibacterial drug albicidin
· Racemization-free synthesis is convergent and easy to scale up (No formation of optical isomers.)
· Strong antibacterial activity with low MIC (minimal inhibitory concentration) values
· Active against quinolone resistant strains
Stage of Development:
Under development/lab tested
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
Patents for China, US and Japan have been granted. Europe and Canada are still pending.

Partner sought

Type and Role of Partner Sought:
The university is looking for Partners from the field of drug development or pharmaceuticals for a license or a research cooperation agreement.

In the framework of a license agreement partners like industry, SMEs or academic would be authorized to use the licensed synthesis route in the process of the further profiling of the drug properties of the substance.

In a research cooperation agreement the partner could be industry, a SME or a university to further develop the technical aspects of the technology in a joint project. The aim should also be the further profiling of the drug properties.

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