Research breakthrough by chemists could enhance drug safety and reduce side effects.
Chemists have successfully addressed a significant challenge in creating a more stable form of heterocycle – a group of organic compounds commonly found in modern pharmaceuticals.
The study, featured in Science, showcases the findings of organic chemists from the University of British Columbia (UBC), the Massachusetts Institute of Technology (MIT), and the University of Michigan. This breakthrough could provide drug developers with more options to enhance medication safety profiles and minimize side effects.
According to Dr. Corinna Schindler, Canada Research Chair in synthetic solutions for bioactive compounds at UBC and the senior author of the paper, “Azetidines, a stable type of heterocycle, have been difficult to synthesize.”
Heterocycles play a crucial role in the formulation of modern drug families, such as cancer drugs and antibiotics, with reports suggesting that 85% of bioactive chemical entities contain a heterocycle.
Unfortunately, many current heterocycles used in pharmaceuticals can oxidize in physiological conditions, leading to unintended effects and impacting medication safety profiles.
Azetidines, characterized by their metabolic stability and resistance to oxidation under physiological conditions, present a promising alternative.
Dr. Schindler expressed hope that this achievement will open doors for researchers to develop new synthetic methods using azetidines with enhanced medical properties.
The research team, led by Dr. Schindler alongside graduate student Emily Wearing at the University of Michigan and in collaboration with Dr. Heather Kulik’s lab at MIT, utilized light-driven reactions and computational techniques to successfully utilize imines in the formation of new azetidines for the first time.
