Chemists have designed a simple way to attach small, strained-ring-shaped chemical groups to potential drug compounds — previously a difficult process.
The structures can change a drug's properties, for example to improve how it is absorbed in the body. Phil Baran at the Scripps Research Institute in La Jolla, California, and his colleagues attached a few such groups — including propellane, which looks like a propeller — to drug molecules by first breaking a high-energy carbon–carbon bond in the ring structure. The team used the energy released from this 'spring-loaded' bond to add another nitrogen-containing molecular group, creating a molecule called an amine. Using their method in a high-throughput synthesis, the team added strained molecules to a range of pharmaceutical compounds.
The team says that scientists in the drug industry have started using the method.
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Spring-loaded bond adds variety. Nature 529, 259 (2016). https://doi.org/10.1038/529259a
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DOI: https://doi.org/10.1038/529259a
