A single nitrogen atom has unlocked new potential in the fields of drug research and development. The findings, which are published in the journal Science, are already gaining attention from drug manufacturers worldwide.
In their research University of Oklahoma researchers demonstrated that by using sulfenylnitrene, a single nitrogen atom can be inserted into bioactive molecules to transform them into new pharmacophores.
"Eighty-five percent of all existing FDA-approved drugs have one or more nitrogen atoms. And when you look at the top 200 brand-name drugs, 75-80% have nitrogen heterocycles," said OU associate professor Indrajeet Sharma. "By selectively adding one nitrogen atom to these existing drug heterocycles in the later stages of development, we can change the molecule's biological and pharmacological properties without changing its functionalities. This could open uncharted regions of chemical space in drug discovery."
While previous research has demonstrated similar concepts, that work required conventional nitrenes and resulted in a large amount of oxidizing agent which was incompatible with many drug molecules. By developing an additive-free sulfenylnitrene production method, the OU researchers have significantly increased the compatibility of the method with other functional groups in the molecule.
"The cost of many drugs depends on the number of steps involved in making them, and drug companies are interested in finding ways to reduce these steps. By adding a nitrogen atom in the late stages of development, you can make new drugs cheaper. It's like renovating a building rather than building it new from scratch," added Sharma.
"Not everyone has equal access to health care. Even in the United States, per capita health expenditures increase to over $12,000 per year. By making these drugs easier to produce at large scale, we could reduce the cost of health care for vulnerable populations around the world."