Stefan Schiesser, the Director of Medicinal Chemistry at AstraZeneca, delivered a compelling presentation on accelerating drug discovery. He began by emphasising the often-overlooked importance of synthetic organic chemistry in medicinal chemistry. While artificial intelligence can propose numerous molecules, the ability to synthesise these molecules efficiently is crucial for demonstrating their potential in drug discovery.
Schiesser illustrated his point with two case studies. The first involved developing a new synthetic method for an already known functional group, while the second focused on accessing a novel functional group previously unused in medicinal chemistry due to synthesis challenges. He highlighted the specific challenges posed by biomolecules, such as peptides and proteins, for synthetic transformations. These challenges included the need for methods that do not interfere with peculiar functional groups and the requirement for suitable solvents.
He also discussed the use of automated chemistry, including robotic machinery for pipetting reaction mixtures. This approach, while advantageous, presented specific challenges, such as the need for easy-to-set-up methods and non-corrosive reagents. Schiesser introduced N-CF3 compounds as a novel functional group in medicinal chemistry. Despite initial scepticism about their stability, the study demonstrated that N-CF3 compounds on heterocyclic nitrogens were stable and could offer advantages such as increased metabolic stability and reduced basicity.
Schiesser concluded by emphasising the interplay between synthetic organic chemistry and medicinal chemistry. He noted that new synthetic methods could significantly impact how medicinal chemistry is conducted. He also acknowledged the contributions of his team and collaborators in advancing these methodologies.
