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5

IQ enhances preparation
of diabetes drug,
Alzheimer's and Parkinson's

Professor Fernando Coelho at the Natural Products and Pharmaceuticals Synthesis Laboratory: technique uses abundant and low-cost raw materials (Photos: Antoninho Perri)Presearchers from the Unicamp Institute of Chemistry (IQ), more specifically from the Laboratory for the Synthesis of Natural Products and Drugs (LSPNF), have just developed a new methodology for the preparation of Efaroxan, a drug that can be used in the treatment of diabetes and diseases neurodegenerative diseases such as Alzheimer's and Parkinson's. The method differs from conventional ones by simplifying the synthesis process, increasing product yield and using abundant, low-cost raw materials. The technique, whose patent was requested by the University last July, is in the phase prior to licensing for the production sector.

Institute has already applied for a patent for the new methodology

According to professor Fernando Coelho, coordinator of the LSPNF, the new methodology was developed during research for the master's thesis of one of his supervisees, Gabriel Pinto de Carvalho e Silveira, which will be defended in November. The method used in the Efaroxan preparation process, says the professor, is absolutely original. Without going into details, due to the secrecy that this type of activity requires, he explains that the technique simplifies some of the reactions necessary to obtain the esters or acids used in the production of the drug. It eliminates, so to speak, some stages of the process.

Furthermore, the raw material used in the methodology is abundant and low-cost. “We use as a substrate a derivative of acrylic acid, which is the same material used, for example, in the preparation of lenses for glasses and bathroom curtains”, explains professor Fernando Coelho. Finally, the method developed by the researchers allows for a synthetic yield superior to that obtained through conventional processes. The LSPNF coordinator considers that the results achieved on a laboratory scale allow the technique to be classified as promising. The next step, according to the expert, will be to increase production, which would go from the milligram standard to kilograms. “This transition generally requires some improvements and adaptations, but I don't think we will face any major problems,” he predicts.

As important as generating products and processes that can bring benefits to society, the research carried out at LSPNF has contributed to training human resources of the highest quality. Several of the professionals who passed through the laboratory, assures its coordinator, are working in large companies or teaching at important universities in the country. “This is very gratifying, as we are contributing to both the production of knowledge and the generation of wealth for Brazil”, analyzes the professor.

Challenge - According to Fernando Coelho, research into the Efaroxan preparation process is important because the medicine has a special characteristic. It can be used in medicine to treat different diseases, such as Alzheimer's, Parkinson's and diabetes. “With the increase in the life expectancy of Brazilians, these illnesses tend to become more common among the population. Thus, the development of more effective and cheaper medicines becomes a constant challenge for science. We are striving to contribute to solving this problem,” he says.

The studies carried out at LSPNF have been financed by the São Paulo State Research Support Foundation (Fapesp), the National Council for Scientific and Technological Development (CNPq), an organization of the Ministry of Science and Technology (MCT), and the Support Fund for Teaching and Research (Faep), managed by Unicamp itself. (MAF)


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