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For Immediate Release - July 26, 1999

Swarthmore Research Team Develops Improved Glaucoma Treatment

Student researchers and a professor at Swarthmore College have developed a method for delivering a glaucoma pain-relief drug that could be significantly more effective than products currently on the market.

In two articles to be published this month in the chemistry journal Organic Letters, the Swarthmore researchers report on the development and delivery of compounds called fluorinated sulfonamides, which have the potential to be about 10 times more efficient than conventional treatments. This discovery could lead to more effective glaucoma pain relief and, more broadly, improved methods for delivering drugs to the human body.

The primary researchers on the project are Dr. Ahamindra Jain, visiting assistant professor of chemistry; Jeffrey Doyon, a senior from Lewiston, Maine; and Polina Kehayova, a junior from Sofia, Bulgaria. Also participating in the research are students Gregory Bokinsky, a senior from Portland, Maine; John Huber, a senior from Teaneck, N.J.; Ariss DerHovanessian, a senior from Los Angeles; Christopher Woodrell, a junior from Orange, Calif.; Elizabeth Hansen, a sophomore from Beaver, Pa.; and Patrick Dostal, a sophomore from Bryn Mawr, Pa. Their work is scheduled to appear in the July 29 issue of Organic Letters, a journal of the American Chemical Society.

The research has two primary thrusts. Doyon and Jain are working to improve the fluorinated sulfonamides, which interact with a protein in the eye known as carbonic anhydrase (CA) to relieve pain. Drugs now in use interact less efficiently with this protein, forcing users to apply pain-relieving eye drops three times a day. Meanwhile, because the sulfonamides do not dissolve in water, Jain and Kehayova are perfecting a method of "masking" the pain relief agents to make them water soluble and thus better absorbed by the eye.

Treatments for glaucoma often rely on a sulfonamide that binds to CA. To make more efficient drugs, one needs to identify other interactions between the drug and the protein that aid the binding. The Swarthmore researchers consider fluorinated inhibitors particularly promising because fluorine possesses a set of unique properties that allow it to interact with the protein in novel ways.

Jain believes an understanding of these interactions might be useful in developing better drugs not only for glaucoma but also for many other diseases. "The interaction of these substances with targets in the human body is very exciting," says Jain, who attended medical school before embarking on a research and academic career. "This could lead to new classes of drugs. The delivery mechanism that my students are developing should also have wide applicability for the site-selective treatment of diseases, via photo-triggering of masked inhibitors."

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