Easier Methods for Building New Drugs


carbon-atom-11-largeA new method has been developed to allow scientists to modify organic molecules that will have a significant impact on the possibility for developing new pharmaceuticals, as well as making existing ones better. A Science Daily news article explains that the innovation made by scientists at The Scripps Research Institute (TSRI) has made it easier to modify existing organic compounds through a process where a biologically active functional group is attached to drug molecules. These functional groups initiate activity in the typical small-molecule drug.

During the past half-century, numerous methods have been developed by chemists to add functional groups to carbon atoms. However, one specific type of modification, “meta” C-H activation, has remained out of reach until now. This refers to the temporary attachment of a helper molecule to a single carbon atom in a way so as to cause the helper molecule to extend past the carbon atom closest to the one that is next closest in order to mediate the addition of a functional group.

Jin-Quan Yu, a professor in TSRIs Department of Chemistry and the senior author of the new report in Nature, was responsible for discovering the innovation. Using a method described by Yu and colleagues previously published in a 2012 edition of the science journal Nature, the team devised a helper molecule with a long segment called a nitrile, with the capability of attaching to one of the carbon atoms in the compound and arching over the next-door carbon atom, to swing a palladium atom at its far end back to the targeted carbon atom. The result would be for the palladium atom to act as the catalyst to dislodge the existing atom and enable the new functional group to attach.

As a result of their discovery, Yu is collaborating with Bristol-Myers Squibb pharmaceuticals to use the meta-C-H activation techniques to potentially make new drug compounds.

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