When changing one atom makes molecules better

The development and improvement of pharmaceuticals plays the central role in the ongoing battle against human disease. Organic synthesis is the field that enables these developments as it offers the toolbox to diversify chemical structures. The group of Nuno Maulide, recently named the Scientist of the Year 2018 in Austria, in collaboration with the group of Harald Sitte, has now reported a facile method for the replacement of hydrogen with fluorine in important drug molecules. This new discovery enables the fine-tuning of existing (and potential new) pharmaceuticals to endow them with improved pharmacological properties. The results have been recently published in the renowned journal Nature Chemistry.

The vast majority of pharmaceuticals employed in the treatment of human diseases are of an organic nature, meaning that the active component is a molecule (or a combination of several molecules) that is constituted of carbon and hydrogen atoms. This trait is shared with all living matter, as proteins, sugars, fats and DNA are also based on such hydrocarbon skeletons, differing only by arrangement and their substitution with a relatively small amount of other possible elements (mainly oxygen, nitrogen, sulfur and phosphorus). “Our bodies are nothing else than a large assembly of billions of carbon-made, or in other words, organic molecules”, says Nuno Maulide, recently named Scientist of the Year 2018 in Austria and Professor at the University of Vienna. Owing to this similarity, organic pharmaceuticals are ideally suited to interact with the human body, for example by binding to receptors thereby triggering or inhibiting a desired or undesired function.

Finding the key that best fits the lock

The design of a pharmaceutical molecule targeting a specific interaction with a receptive structure is often conceptualised by the analogy of a lock and key. “The receptor (for example an enzyme) has a unique structure (lock) and therefore requires a unique structure (key) to interact with. Due to the need for an exact fit, the structural integrity of the pharmaceutical compound is key (pun intended!) to assure its beneficial bioactivity”, explains Harald Sitte, Professor at the Medical University of Vienna and co-author of the study.

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