The National Centre for Research and Development

  Project title

Synthesis and assessment of the activity of new ligands acting on central nervous system (CNS) receptors

  Name of Beneficiary/Beneficiaries

Tadeusz Kościuszko Krakow University of Technology, Project Manager – PhD. Eng. Jolanta Jaśkowska

  Name of programme

National programmes

  Competition

LIDER VI

  Project value

PLN 1,200,000

  Funding value

PLN 1,200,000

  Project delivery period

15.04.2016 - 14.04.2019

Get to know our team

Team

• PhD. Eng. Jolanta Jaśkowska - Project manager
• MSc.Eng. Damian Kułaga
• MSc.Eng. Anna K. Drabczyk
• PhD. Eng. Magdalena Malinowska
• PhD. Grzegorz Satała
• DSc. Łukasz Szeleszczuk
• PhD. Eng. Paweł Śliwa
• DSc. Eng Bożena Tyliszczak
• PhD. Eng. Przemysław Zaręba

the characteristics of the team can be found on the project website: http://ligandy-lider.pk.edu.pl/

See the effect of our work

As part of the project, we and our team have developed and patented three new paths for the synthesis of bioactive compounds: by microwave radiation, in the presence of ultrasound and a mechanochemical method. Initially, we adapted these methods to the synthesis of compounds with potential antidepressant activity, then we confirmed the universality of these methods also in the synthesis of anticancer, antibacterial and antiviral compounds.

While implementing the project, we obtained several hundred compounds with potential antidepressant activity, of which we managed to confirm in vitro and in vivo activity among several of them. Interestingly, some molecules have a very selective effect on key serotonin and dopamine receptors, which means that they can be considered as molecules for further development towards the search for new drugs.

The results of the work were covered by 6 patents, described in 10 international publications and presented during numerous scientific conferences and invention exhibitions.

 

List of awards related to project no. LIDER/015/Ln 6/14/NCBR/2015:

1. GOLD MEDAL at the 11th International Warsaw Invention Exhibition IWIS 2017, which took place on October 9-12, 2018 at the Warsaw University of Technology.

2. Distinction of the Polish Chamber of Chemical Industry for the invention "A New Universal Solvent-Free Method For The Synthesis Of Active Substances On The Example Of Aripiprazole" - IWIS 2017, 9 12/10/2018

3. SPECIAL AWARD, SPECJAL AWARD INNOVATORENPREIS Forschungsinstitut fur Erfinderforderung, Innovationen und Netzwerkmanagment for the invention "Method for obtaining trazodone", during the International trade fair for "Ideas - Inventions - New Products" IENA, Nuremberg, Germany, 2-5/11/2017

4. GOLD MEDAL - for the invention "Method of obtaining trazodone", during the 15th International Innovation Exhibition ARCA 2017, Zagreb, Croatia, October 19-21, 2017

5. SILVER MEDAL - for the invention "Method of obtaining trazodone", during the 11th International 

Warsaw Invention Exhibition, IWIS 2017, Warsaw, October 9-11, 2017

6. HONORABLE MENTION - for the invention "Method of obtaining trazodone" Taipei International Invention Show & Technomart Invention Contest, Taipei, Taiwan, September 28-30, 2017

7. BRONZE MEDAL during the Korea International Women's Invention Exposition 2017 (KIWIE 2017) for the invention "Method of obtaining aripiprazole" 8-11/06/2017

8. Special award of the Polish Chamber of Chemical Industry in the 5th International Chemical Competition organized jointly by the International Federation of Associations of Inventors IFIA and the Association of Polish Inventors and Rationalizers for "Development of a new method for obtaining long-chain arylpiperazines (LCAPs) under the influence of microwave radiation". The award was presented during the 10th International Warsaw Invention Exhibition on October 10-12, 2016.

9. Silver medal at the 10th International Warsaw Invention Exhibition IWIS 2016, which took place on October 10-12, 2016 at the Warsaw University of Technology.

 

Videos, broadcasts and articles about the project can be found at the links below:

What problem does our project solve?

The aim of the project entitled "Synthesis and assessment of the activity of new ligands acting on central nervous system (CNS) receptors" was to obtain new compounds with potential activity towards diseases related to disorders of the central nervous system. As a result of the project, a group of compounds was obtained that has positive prospects for further development as a potential antidepressant drug. Moreover, the project developed three new synthesis methods that allow obtaining high-purity bioactive compounds in a short time, e.g. within 60 seconds in the presence of microwave radiation. An additional advantage is the fact that these methods are environmentally friendly because they eliminate the use of toxic reagents and solvents and significantly reduce energy consumption compared to classical synthesis methods. Thanks to the above-mentioned advantages, the developed methods can be successfully classified as the so-called green chemistry.

Who will benefit from the project results?

The subject of potential implementation are both new methods for the synthesis of bioactive compounds as well as groups of compounds with precisely defined activity towards selected key receptors in the treatment of diseases of the central nervous system. The beneficiaries may therefore be pharmaceutical companies and companies involved in the synthesis of bioactive compounds.

What was the biggest challenge for us in implementing the project?

The biggest challenge during the project was to develop synthesis methods that would allow obtaining high-purity bioactive compounds in a short time. The work carried out proved that the developed methods are not only effective in synthesis but also ecological due to the possibility of eliminating solvents or the possibility of replacing toxic organic solvents, e.g. with water.

Our advice to other Applicants

Our advice to other Applicants? It's worth dreaming and trying new things, even if at first you hear many times that these are daydreams. Initially, we heard many times that the syntheses currently protected by patents were impossible to achieve... Our research proved that not only are they possible, but they can also be appropriately modified to increase their versatility to obtain compounds with high structural diversity. .