New reaction will make indoline scaffolds available for pharmaceutical development

ScienceDaily | 9/23/2019 | Staff
ajoy26 (Posted by) Level 3
One of them -- Prof. Donald A. Watson -- is part of the Department of Chemistry and Biochemistry where Heck taught during his time on UD's faculty (1971-89). And Watson and his research group have just published new findings that could streamline development and production of small-molecule pharmaceuticals, which comprise the majority of medicines in use today. The active ingredients in these small-molecule drugs are typically delivered by a tablet or capsule and absorbed into the bloodstream.

Their work, published in Angewandte Chemie, shows how the Heck Reaction (which uses palladium as a catalyst to bond carbon molecules) can make it easier and more practical to produce indoline scaffolds -- structures that provide an important platform for new molecules.

Indoline - Scaffolds - Products - Medicines - Diseases

Indoline scaffolds are found in many natural products as well as medicines used to treat diseases including cancer, hypertension, migraine headaches and other conditions.

But producing these scaffolds has been challenging, especially when more complexity is required.

Watson - Group - Way - Heck - Reaction

Watson and his group saw a new way to deploy the Heck Reaction, using nitrogen, an electron-craving element, to accomplish the assembly in previously unattempted ways and make complex assemblies accessible. With nitrogen as a reagent -- the element that governs the chemical reaction -- new possibilities emerged.

"Everything Heck focused on is based on carbon-based reagents," Watson said. "We are asking, can this be applied to other elements in the periodic table? The answer to that in short is yes. That's what we're finding... We have looked at silicon, boron atoms and, now, nitrogen, which is directly relevant to the fabrication of bioactive compounds."

Compound - Response - Living - Organism - Compounds

A bioactive compound is used to provoke a specific biological response in a living organism. The bioactive compounds in medicines, for example, may be used to kill bacteria, lower blood pressure or kill cancer cells.

Watson credits doctoral student Feiyang Xu, the lead author of the...
(Excerpt) Read more at: ScienceDaily
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