Nav: Home

Seeking a better way to design drugs

September 23, 2015

Worcester, Mass. - The National Institutes of Health (NIH) has awarded $346,000 to Worcester Polytechnic Institute (WPI) for a three-year research project to advance development of a chemical process that could significantly improve the ability to design new pharmaceuticals and streamline the manufacturing of existing drugs.

Led by Marion Emmert, PhD, assistant professor of chemistry and biochemistry at WPI, the research program involves early-stage technology developed in her lab that may yield a more efficient and predictable method of bonding a vital class of structures called aromatic and benzylic amines to a drug molecule.

"Seven of the top 10 pharmaceuticals in use today have these substructures, because they are so effective at creating a biologically active compound," Emmert said. "The current processes used to add these groups are indirect and not very efficient. So we asked ourselves, can we do it better? "

For a drug to do its job in the body it must interact with a specific biological target and produce a therapeutic effect. First, the drug needs to physically attach or "bind" to the target, which is a specific part of a cell, protein, or molecule. As a result, designing a new drug is like crafting a three-dimensional jigsaw puzzle piece that fits precisely into an existing biological structure in the body. Aromatic and benzylic amines add properties to the drug that help it bind more efficiently to these biological structures.

Getting those aromatic and benzylic amines into the structure of a drug, however, is difficult. Traditionally, this requires a specialized chemical bond as precursor in a specific location of the drug's molecular structure. "The current approach to making those bonds is indirect, requires several lengthy steps, and the outcome is not always precise or efficient," Emmert said. "Only a small percentage of the bonds can be made in the proper place, and sometimes none at all."

Emmert's new approach uses novel reagents and metal catalysts to create a process that can attach amines directly, in the right place, every time. In early proof-of-principle experiments, Emmert has succeeded in making several amine bonds directly in one or two days, whereas the standard process can take two weeks with less accuracy. Over the next three years, with support from the NIH, Emmert's team will continue to study the new catalytic processes in detail. They will also use the new process to synthesize Asacol, a common drug now in use for ulcerative colitis, and expect to significantly shorten its production.

"Some of our early data are promising, but we have a lot more work to do to understand the basic mechanisms involved in the new processes," Emmert said. "We also have to adapt the process to molecules that could be used directly for drug development."
-end-
About Worcester Polytechnic Institute

Founded in 1865 in Worcester, Mass., WPI is one of the nation's first engineering and technology universities. Its 14 academic departments offer more than 50 undergraduate and graduate degree programs in science, engineering, technology, business, the social sciences, and the humanities and arts, leading to bachelor's, master's and doctoral degrees. WPI's talented faculty work with students on interdisciplinary research that seeks solutions to important and socially relevant problems in fields as diverse as the life sciences and bioengineering, energy, information security, materials processing, and robotics. Students also have the opportunity to make a difference to communities and organizations around the world through the university's innovative Global Perspective Program. There are now 45 WPI project centers in the Americas, Africa, Asia-Pacific, and Europe.

Worcester Polytechnic Institute

Related Pharmaceuticals Articles:

Study describes cocktail of pharmaceuticals in waters in Bangladesh
An analysis revealed that water samples held a cocktail of pharmaceuticals and other compounds, including antibiotics, antifungals, anticonvulsants, anesthetics, antihypertensive drugs, pesticides, flame retardants and more.
Treating wastewater with ozone could convert pharmaceuticals into toxic compounds
With water scarcity intensifying, wastewater treatment and reuse are gaining popularity.
Study calls for improved sanitation and the environmental management of pharmaceuticals
Failure to ensure the environmental sustainability of growing patient access to medicines in developing economies could increase the risk of adverse environmental impacts, according to new research led by the University of Plymouth.
Chemicals for pharmaceuticals could be made cheaper and greener by new catalysts
High value chemicals used to make pharmaceuticals could be made much cheaper and quicker thanks to a series of new catalysts made by scientists at the University of Warwick in collaboration with GoldenKeys High-Tech Co., Ltd. in China.
Soaking up pharmaceuticals and personal care products from water
Medications excreted in the urine or dumped into the toilet can end up in the water supply, just like lotions or cosmetics that wash off the body and go down the sink or shower drain.
New study finds river wildlife contain cocaine, pharmaceuticals and pesticides
For the first time, researchers at King's College London, in collaboration with the University of Suffolk, have found a diverse array of chemicals, including illicit drugs and pesticides in UK river wildlife.
Metal-free catalyst to convert aldehyde into ketone, a basic structure of pharmaceuticals
We succeeded in synthesizing a ketone, a basic structure of many pharmaceuticals, from an aldehyde and a carboxylic acid using N-heterocyclic carbene catalyst under mild conditions.
Human pharmaceuticals change cricket personality
Crickets that are exposed to human drugs that alter serotonin levels in the brain are less active and less aggressive than crickets that have had no drug exposure, according to a new study led by researchers from Linköping University.
Screen strategies for off-target liability prediction & ID small-molecule pharmaceuticals
A new review in SLAS Discovery explores how improved safety screening strategies and methods are improving the pharmaceutical discovery and development process.
Small amounts of pharmaceuticals found in north central Pa. rural well water
Drinking water from wells in rural north central Pennsylvania had low levels of pharmaceuticals, according to a study led by Penn State researchers.
More Pharmaceuticals News and Pharmaceuticals Current Events

Trending Science News

Current Coronavirus (COVID-19) News

Top Science Podcasts

We have hand picked the top science podcasts of 2020.
Now Playing: TED Radio Hour

Listen Again: Reinvention
Change is hard, but it's also an opportunity to discover and reimagine what you thought you knew. From our economy, to music, to even ourselves–this hour TED speakers explore the power of reinvention. Guests include OK Go lead singer Damian Kulash Jr., former college gymnastics coach Valorie Kondos Field, Stockton Mayor Michael Tubbs, and entrepreneur Nick Hanauer.
Now Playing: Science for the People

#562 Superbug to Bedside
By now we're all good and scared about antibiotic resistance, one of the many things coming to get us all. But there's good news, sort of. News antibiotics are coming out! How do they get tested? What does that kind of a trial look like and how does it happen? Host Bethany Brookeshire talks with Matt McCarthy, author of "Superbugs: The Race to Stop an Epidemic", about the ins and outs of testing a new antibiotic in the hospital.
Now Playing: Radiolab

Dispatch 6: Strange Times
Covid has disrupted the most basic routines of our days and nights. But in the middle of a conversation about how to fight the virus, we find a place impervious to the stalled plans and frenetic demands of the outside world. It's a very different kind of front line, where urgent work means moving slow, and time is marked out in tiny pre-planned steps. Then, on a walk through the woods, we consider how the tempo of our lives affects our minds and discover how the beats of biology shape our bodies. This episode was produced with help from Molly Webster and Tracie Hunte. Support Radiolab today at Radiolab.org/donate.