Researchers Develop Green Method for Active Pharmaceutical Ingredient Synthesis

 Researchers Develop Green Method for Active Pharmaceutical Ingredient Synthesis

Researchers have recently developed a novel method for active pharmaceutical ingredient synthesis that does not rely on any harmful starting materials. The method presents a more sustainable alternative method to traditional manufacturing that involves environmentally harmful reagents or materials.

In the research, published in Angewandte Chemie, researchers from the University of Graz and the Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) developed a novel method utilizing wood waste for the synthesis of active pharmaceutical ingredients (API). By utilizing lignin, a biopolymer found in plants and one of the most abundant organic compounds found worldwide, the researchers were able to use only biodegradable solvents and reagents for API production. 

After conversion into multiple classes of potential active substances, the lignin-based products were then assessed for their biological activity. "In characterizing our synthesized molecules, we looked at which of the substances were capable of influencing the growth of different types of bacteria, or even cancer cells," said Anna Hirsch head of the Drug Design and Optimization department at HIPS and professor of medicinal chemistry at Saarland University. "We were pleasantly surprised: Several of the candidates produced showed excellent activity, even against germs that often show resistance to common antibiotics in a clinical context and thus cause major problems. This shows us that our strategy is quite capable of addressing the need for new compounds."

One of the most promising compounds has already been evaluated and has shown efficacy when used in an infection model for larvae of large wax moths. In testing, the survival rate of wax moths infected with Streptococcus pneumoniae, a pathogen that causes pneumonia in humans, was significantly increased after treatment with the compound produced by the researchers. 

 "Our technology allows us to produce molecules that are otherwise very difficult to access—and on the basis of a substance that would normally be considered waste," said Katalin Barta, professor of bioorganic chemistry at the University of Graz. "We are certain that production processes of the future will have to be green and sustainable. Already today, there is a critical shortage of resources in some parts of pharmaceutical production. So if we manage to offer an economically viable alternative based on lignin, we can address two problems at once."

Current methods of producing active ingredients rely on petroleum-based reagents, further increasing our reliance on fossil fuels. The researchers are hopeful that their methods could reduce that reliance and plan to further optimize their compounds for production.


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