Creating Drug 'Skeletons' Using Visible Light

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[Asia Economy Reporter Junho Hwang] The medicines we commonly take are composed of low-molecular compounds consisting of a 'framework' like a tree trunk and 'functional groups' attached as branches. Functional groups bind to molecules such as proteins or nucleic acids in the body to enhance or inhibit their functions, producing therapeutic effects.

However, for a drug to exert its therapeutic effect, it must have a very precise and specific molecular structure. This is because the drug must pass through the complex body and reach the treatment site. Accordingly, the scientific community is conducting research to synthesize more sophisticated low-molecular compounds than existing drugs for use as medicines. In particular, methods utilizing low temperature, low pressure, and low energy are being studied, and domestic researchers have developed a technology that can create the drug framework using visible light.

Constructing Drug Frameworks with Visible Light

Professor Cheolmin Park's research team at the School of Natural Sciences, Ulsan National Institute of Science and Technology (UNIST), announced on the 11th that they succeeded in synthesizing cyclobutene compounds using visible light and photocatalysts.

Cyclobutene is a framework that is difficult to synthesize. This substance consists of four carbon atoms arranged in a square ring structure, but the ring's strain is unstable, making it difficult to synthesize with various functional groups. Although synthesis is possible using ultraviolet light, the high energy of UV light affects the functional groups, making it hard to form the desired drug structure.

The research team developed a technology to synthesize cyclobutene compounds using blue visible light and an iridium (Ir) photocatalyst. The efficiency reaches 99%, and the technology allows the addition of various functional groups.

Researcher Sujin Ha said, "We succeeded in synthesizing cyclobutene by utilizing the ring addition reaction (a reaction forming a ring shape) between alkene with two carbon atoms double-bonded and alkyne with a triple bond." The team explained that the iridium photocatalyst, excited by the energy of visible light, first activates the electrons of the alkene, enabling the construction of cyclobutene compounds.

Possibility of Chemical Product Development

The research team also synthesized a 1,3-diene framework using this technology. They sequentially induced the ring-forming reaction and the ring-opening reaction to construct 1,3-diene with coumarin and 2-quinolone as functional groups. The 1,3-diene framework is a compound applied in actual drugs and sensor materials. Coumarin is a natural substance with hemostatic effects, and 2-quinolone is an isomer of 4-quinolone, the raw material for quinolone antibiotics.

Professor Cheolmin Park said, "Through this research, we developed a new synthesis method for cyclobutene, a core structure of various drugs and natural substances. Using the developed synthesis method, it is possible to create cyclobutene frameworks with various functional groups, which can be used not only for drugs but also for the development of various chemical products."

The research results were published in the international journal Nature Communications.

This content was produced with the assistance of AI translation services.